Ch1 introduction to medicinal chemistry
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Medicinal chemistry is an interdisciplinary science that combines chemistry, biology, and pharmacology. It involves the design and development of new chemical entities for use as pharmaceuticals. The key steps include discovering lead compounds through screening of natural or synthetic substances, optimizing lead compounds to improve potency and selectivity, and developing lead compounds into drug candidates with suitable pharmacokinetic properties. Drugs can come from natural sources like plants and animals, or be synthesized chemically. They are classified based on their chemical structure, pharmacological action, or the diseases they treat. Drug names include chemical names based on structure, generic names assigned by regulators, and proprietary brand names given by manufacturers.
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Medicinal chemistry
Medicinal chemistry involves the design and synthesis of pharmaceutical agents to benefit humanity. It includes structure-activity relationships, receptor interactions, and absorption/metabolism properties of compounds. Combinatorial chemistry produces large libraries of similar molecules for screening via techniques like solid phase synthesis and parallel/mixed synthesis. Quantitative structure-activity relationship analysis uses parameters like lipophilicity, electronic effects, and steric hindrance to develop mathematical models correlating biological activity to a compound's physicochemical properties.
Introduction To Medicinal Chemistry
This is the presentation for B. Pharm. IV semester students.
It includes Introduction of Medicinal Chemistry, History and Development of Medicinal Chemistry
History of Medicinal Chemistry
Medicinal chemistry involves the design and synthesis of pharmaceutical agents to benefit humanity. It includes synthesis, structure-activity relationship studies, receptor interactions, and analysis of absorption, distribution, metabolism, and excretion. The field has its roots in the isolation of alkaloids like morphine in the early 19th century. In the late 19th century, semi-synthetic and synthetic derivatives of plant-derived compounds were developed. Modern medicinal chemistry emerged in the late 19th/early 20th century with advances like the receptor theory and development of antibiotics and sulfonamides. The 1940s-1960s were a "golden era" with the invention of many modern drug classes such as corticosteroids, antipsychotics
1 UNIT I: INTRODUCTION TO MEDICINAL CHEMISTRY
Medicinal chemistry is a multidisciplinary field that combines organic chemistry, biochemistry, pharmacology and other sciences to study the design, synthesis and actions of pharmaceutical drugs. The document provides a brief history of medicinal chemistry, noting early examples of medicinal substances used in ancient civilizations. It then discusses several important physicochemical properties that influence a drug's biological effects, including solubility, partition coefficient, hydrogen bonding, ionization and others. The relationships between these properties and drug absorption, distribution, metabolism and excretion are also summarized.
Sorces of crude drugs
Drugs are obtained from six major sources: plant sources, animal sources, mineral/earth sources, microbiological sources, semi-synthetic sources, and recombinant DNA technology. Plant sources provide most drugs in ancient times and include leaves, stems, bark, fruits, and roots of plants. Animal sources include organs and fluids like the pancreas, urine, thyroid, cod liver, pituitary gland, and blood. Mineral sources consist of metals and non-metals like iron, mercury, zinc, iodine, and gold. Microbiological sources include fungi, bacteria, and other microorganisms. Semi-synthetic drugs have a natural source nucleus but an altered chemical structure. Recombinant DNA involves inserting genes into bacteria
Importance of Stereochemistry manik
1. The document discusses the importance of stereochemistry in pharmacy. Biological systems often have a preference for specific stereoisomers of drugs. For example, only the L-forms of amino acids are used in protein synthesis.
2. Drug efficacy, side effects, and toxicity can be stereospecific. Only one enantiomer of drugs like statins are used clinically as the "eutomer", while the other "distomers" may not have the desired effects or could even be harmful.
3. Biological receptors like enzymes are also chiral and will only interact with one stereoisomer of a drug. This is why drugs are often administered as single enantiomers rather than racemic mixtures.
Medicinal chemistry i
Medicinal chemistry involves the discovery and design of new therapeutic chemicals and their development into medicines and drugs. It is an interdisciplinary field combining chemistry and biology. Medicinal chemists work to design new drug compounds, determine their biological effects, optimize their structures for desired effects and minimal side effects, and study how the body processes drugs. The physicochemical properties of drugs, like solubility, acidity, and reactivity influence their biological actions and interactions with targets in the body. Understanding these properties helps predict drugs' behaviors and design new candidates. A drug's solubility is key to its formulation and absorption in the body. Both lipophilic and hydrophilic structural features impact a molecule's solubility profile. Acidity and
Synthesis of some important drugs
The document outlines the units and topics covered in a course on Medicinal Chemistry-I. Unit II discusses the synthesis of drugs acting on the autonomic nervous system including Tolazoline, Salbutamol, Phenylephrine, and Propranolol. Unit III covers drugs acting on the cholinergic nervous system such as Neostigmine, Dicyclomine Hydrochloride, Carbachol, and Ipratropium bromide. Units IV and V address drugs acting on the central nervous system, listing substances like Diazepam, Chlorpromazine, Ethosuximide, and others.
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Medicinal chemistry
Medicinal chemistry involves the design and synthesis of pharmaceutical agents to benefit humanity. It includes structure-activity relationships, receptor interactions, and absorption/metabolism properties of compounds. Combinatorial chemistry produces large libraries of similar molecules for screening via techniques like solid phase synthesis and parallel/mixed synthesis. Quantitative structure-activity relationship analysis uses parameters like lipophilicity, electronic effects, and steric hindrance to develop mathematical models correlating biological activity to a compound's physicochemical properties.
Introduction To Medicinal Chemistry
This is the presentation for B. Pharm. IV semester students.
It includes Introduction of Medicinal Chemistry, History and Development of Medicinal Chemistry
History of Medicinal Chemistry
Medicinal chemistry involves the design and synthesis of pharmaceutical agents to benefit humanity. It includes synthesis, structure-activity relationship studies, receptor interactions, and analysis of absorption, distribution, metabolism, and excretion. The field has its roots in the isolation of alkaloids like morphine in the early 19th century. In the late 19th century, semi-synthetic and synthetic derivatives of plant-derived compounds were developed. Modern medicinal chemistry emerged in the late 19th/early 20th century with advances like the receptor theory and development of antibiotics and sulfonamides. The 1940s-1960s were a "golden era" with the invention of many modern drug classes such as corticosteroids, antipsychotics
1 UNIT I: INTRODUCTION TO MEDICINAL CHEMISTRY
Medicinal chemistry is a multidisciplinary field that combines organic chemistry, biochemistry, pharmacology and other sciences to study the design, synthesis and actions of pharmaceutical drugs. The document provides a brief history of medicinal chemistry, noting early examples of medicinal substances used in ancient civilizations. It then discusses several important physicochemical properties that influence a drug's biological effects, including solubility, partition coefficient, hydrogen bonding, ionization and others. The relationships between these properties and drug absorption, distribution, metabolism and excretion are also summarized.
Sorces of crude drugs
Drugs are obtained from six major sources: plant sources, animal sources, mineral/earth sources, microbiological sources, semi-synthetic sources, and recombinant DNA technology. Plant sources provide most drugs in ancient times and include leaves, stems, bark, fruits, and roots of plants. Animal sources include organs and fluids like the pancreas, urine, thyroid, cod liver, pituitary gland, and blood. Mineral sources consist of metals and non-metals like iron, mercury, zinc, iodine, and gold. Microbiological sources include fungi, bacteria, and other microorganisms. Semi-synthetic drugs have a natural source nucleus but an altered chemical structure. Recombinant DNA involves inserting genes into bacteria
Importance of Stereochemistry manik
1. The document discusses the importance of stereochemistry in pharmacy. Biological systems often have a preference for specific stereoisomers of drugs. For example, only the L-forms of amino acids are used in protein synthesis.
2. Drug efficacy, side effects, and toxicity can be stereospecific. Only one enantiomer of drugs like statins are used clinically as the "eutomer", while the other "distomers" may not have the desired effects or could even be harmful.
3. Biological receptors like enzymes are also chiral and will only interact with one stereoisomer of a drug. This is why drugs are often administered as single enantiomers rather than racemic mixtures.
Medicinal chemistry i
Medicinal chemistry involves the discovery and design of new therapeutic chemicals and their development into medicines and drugs. It is an interdisciplinary field combining chemistry and biology. Medicinal chemists work to design new drug compounds, determine their biological effects, optimize their structures for desired effects and minimal side effects, and study how the body processes drugs. The physicochemical properties of drugs, like solubility, acidity, and reactivity influence their biological actions and interactions with targets in the body. Understanding these properties helps predict drugs' behaviors and design new candidates. A drug's solubility is key to its formulation and absorption in the body. Both lipophilic and hydrophilic structural features impact a molecule's solubility profile. Acidity and
Synthesis of some important drugs
The document outlines the units and topics covered in a course on Medicinal Chemistry-I. Unit II discusses the synthesis of drugs acting on the autonomic nervous system including Tolazoline, Salbutamol, Phenylephrine, and Propranolol. Unit III covers drugs acting on the cholinergic nervous system such as Neostigmine, Dicyclomine Hydrochloride, Carbachol, and Ipratropium bromide. Units IV and V address drugs acting on the central nervous system, listing substances like Diazepam, Chlorpromazine, Ethosuximide, and others.
Alkaloids
The document discusses alkaloids, which are basic nitrogenous plant compounds that are physiologically active. It defines alkaloids and describes their distribution in plants, forms, nomenclature, extraction and classification. Key points include that alkaloids are found mainly in dicots and families like Apocynaceae, with properties like being crystalline solids, bitter taste, and soluble in organic solvents but not water. Common tests for alkaloids are Mayer's, Dragendorff's, Wagner's and Hager's tests. Alkaloids are classified based on their biogenetic pathway, plant source, basic chemical skeleton or type of amine group.
Nomenclature of optical isomerism
The document discusses the representation and nomenclature of optical isomers. It defines:
- Wedge and dash projection and Fischer projection for representing 3D structures in 2D.
- The D/L and R/S systems for assigning configuration to chiral centers. The D/L system uses hydroxy acid/amino acid and sugar conventions while the R/S system uses Cahn-Ingold-Prelog priority rules.
- Sequence rules for assigning priority to groups around a chiral center in the R/S system.
- Methods for determining R/S configuration including orientation of the lowest priority group and interchanging groups in Fischer projections.
SAR of Morphine
This document discusses structure-activity relationships in drug design and formulation. It introduces Hammett and Hansch plots, which relate reaction rates and biological activity to electronic and physicochemical properties. Modification of lead compounds is explored through changing functional groups, stereochemistry and lipophilicity. Morphine is used as a case study to illustrate how properties like log P, binding groups and stereochemistry impact opioid activity. The conclusion emphasizes the role of medicinal chemistry in understanding disease and developing safer, more effective pharmaceuticals.
Alkaloids
- Alkaloids are basic nitrogen-containing compounds that are often obtained from plants and demonstrate physiological effects.
- They are classified based on their biological origin, biosynthetic pathway, chemical structure, and pharmacological effects.
- Common alkaloids include morphine, quinine, caffeine, and nicotine. They are extracted from plants using various organic solvents and purified.
Medicinal chemistry
This is a ppt on Medicinal chemistry, just made to help out and give the students of CLASS XI studying in CBSE about what Medicinal Chemistry is >>Please do feedback in the comments part
Organized crude drug and unorganized crude drug
This document summarizes organized and unorganized crude drugs. It defines crude drugs as substances obtained from natural sources like plants, animals, and minerals that are used as is without processing except drying and size reduction. Organized crude drugs are obtained from definite anatomic parts of plants like flowers and leaves, have a cellular structure, and are solid. Unorganized crude drugs do not have a cellular structure, can be solid, semisolid or liquid, and are identified through chemical and physical tests rather than microscopic examination. Examples of each type are provided.
Tropane alkaloids notes
This document discusses tropane alkaloids, specifically atropine alkaloid. It summarizes that atropine alkaloid is mainly found in plants from the solanaceae family, like Atropa belladona and Datura stromonium. It then describes the isolation, biosynthesis, identification tests, chemistry and properties, structure-activity relationships, uses, and mechanism of action of atropine alkaloid.
Alkaloids
This document discusses alkaloids, which are nitrogenous plant compounds that have physiological effects. It describes their characteristics, sources, uses, and importance in pharmacy. Key points include: alkaloids are bitter and derived from amino acids; sources include various plant families; uses include analgesic, narcotic, and mydriatic effects; important alkaloids include morphine, codeine, nicotine, and atropine. Tests are outlined to identify the presence of alkaloids. The document also classifies and describes important alkaloid groups such as tropane and solanaceous alkaloids.
Basic metabolic
This document provides an overview of basic metabolic pathways in plants. It discusses primary and secondary metabolism, the role of enzymes and co-enzymes, and several key pathways such as the shikimic acid, acetate, and mevalonate pathways. Primary metabolites such as starch, cellulose, and chlorophyll are synthesized through basic metabolic pathways and are essential for plant growth and function. Secondary metabolites are derived from primary metabolites and have pharmacological activities. Enzymes help catalyze biochemical reactions in metabolic pathways, while co-enzymes assist enzymes and participate in reactions. Biosynthesis converts carbon dioxide into carbohydrates through photosynthesis.
ANTIBIOTICS[PENICILLINS] MEDICINAL CHEMISTRY BY RAVISANKAR
ANTIBIOTICS[PENICILLINS} MEDICIANL CHEMISTRY BY P.RAVISANKAR
VIGNAN PHARMACY COLLEGE
VADLAMUDI
GUNTUR- A.P
INDIA
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Bioisosterism is a strategy used in drug design that involves replacing one chemical group with another that has similar physical or chemical properties. This is done to improve properties like potency, selectivity, toxicity, and pharmacokinetics without significantly changing the chemical structure. Common bioisosteric replacements include replacing hydrogen with fluorine, replacing carboxylic acids with amides or esters, or replacing phenyl rings with heteroaromatic or saturated rings. The application of bioisosterism has been an important concept in medicinal chemistry for nearly 80 years and will continue to play a role in drug discovery and optimization.
Medicinal chemistry-Anticancer agents
The document discusses various types of anticancer agents, including their classification and mechanisms of action. It focuses on alkylating agents, specifically nitrogen mustards. Nitrogen mustards were some of the first chemicals used to treat cancer and work by alkylating DNA at the N7 position of guanine. This prevents replication and can activate apoptosis. Examples discussed include mechlorethamine, chlorambucil, melphalan, and cyclophosphamide. Cyclophosphamide must be activated in the body to form an aziridinium ion that alkylates DNA. The document also briefly mentions mitomycin C, an antibiotic used in cancer treatment.
Qsar
QSAR attempts to correlate biological activity to measurable physicochemical properties through mathematical equations. It relates parameters like lipophilicity (log P), electronic effects (Hammett constants), and steric effects to biological response. Various QSAR methods exist, including Hansch analysis which uses these substituent constants in its equations. More advanced techniques like CoMFA analyze fields around aligned molecules to model activity landscapes and identify favorable regions for activity. QSAR provides a framework for drug design and predicting activities of untested compounds.
Antimalarial drugs
Natural compounds from the bark of the cinchona tree, most notably quinine was observed to exhibit antimalarial activity.
Until the development of synthetic derivatives (ie. 4-aminoquinoline antimalarials), quinine continued to be the first choice to treat malaria.
Quinine is associated with side effects such as diarrhœa.
4-aminoquinoline antimalarials such as amodiaquine and chloroquine largely replaced quinine because of reduced unpleasant side effects.
The life cycle of the parasite and the immunological defence mechanisms against the parasite are complex.
Part of the parasite’s life cycle involves invasion of red blood cells (erythrocytes).
The haemoglobin within the red blood cell is broken down by the parasite and is used as a source of amino acids.
The 4-aminoquinolines act at the erythrocytic stage of the parasite.
Doxycycline is a compound used in prophylaxis against plasmodial parasites.
Other compounds associated with treating malaria include halofantrine and lumefantrine, often used in combination with other drugs.
Urinary tract anti-infective agent
This document discusses urinary tract infections and various quinolone antibiotics used to treat them. It begins by defining urinary tract infections, distinguishing between lower UTI (cystitis) affecting the bladder and upper UTI (pyelonephritis) affecting the kidneys. Symptoms of lower UTI include pain and frequent urination, while upper UTI additionally causes fever and flank pain. The document then introduces quinolone antibiotics, which are broad-spectrum antibiotics containing a fluoroquinolone. Examples mentioned include ciprofloxacin, levofloxacin, and ofloxacin. The mechanisms of action and classifications of various quinolone generations are briefly outlined. Specific quin
Anticholinergic agent
This document summarizes cholinergic antagonists, which are drugs that block the effects of acetylcholine in the muscarinic receptor. It discusses their structure-activity relationships, medical uses in conditions like ulcers, overactive bladder, and organophosphate poisoning. Specific antagonists are described like atropine, hyoscyamine, scopolamine, ipratropium, tiotropium, benztropine, biperiden, tropicamide, and others. Their mechanisms of action, pharmacological effects, and clinical applications are concisely outlined.
Definition, historical landmarks, scope of pharmacology
This presentation highlights Definition, historical landmarks & scope of pharmacology. It also includes essential medicines.
Alkaloids Pharmacognosy
The document provides information about a presentation on alkaloids. It discusses that alkaloids are basic nitrogen-containing compounds found mainly in plants. They have a complex molecular structure and show significant pharmacological activity. Alkaloids are classified based on whether the nitrogen is part of a ring or not. They exhibit diverse physical and chemical properties and are tested using various chemical reagents like Mayer's reagent. Alkaloids have many uses as analgesics, antihypertensives, and in treating other medical conditions due to their pharmacological activities. Examples of alkaloid-containing plants discussed include Lobelia, which has expectorant properties.
Tetracycline sar
-a broad-spectrum antibiotics.
-It is commonly used to treat acne, infection, and other infections caused by bacteria.
-The first of these compounds was chlortetracycline followed by oxytetracycline and tetracycline.
Tetracycline is a broad-spectrum polyketide antibiotic produced by the Streptomyces genus of Actinobacteria, indicated for use against many bacterial infections. It is a protein synthesis inhibitor. It is commonly used to treat acne today, and, more recently, rosacea, and is historically important in reducing the number of deaths from cholera. Tetracycline is marketed under the brand names Sumycin, Tetracyn, and Panmycin, among others. Actisite is a thread-like fiber formulation used in dental applications. It is also used to produce several semisynthetic derivatives, which together are known as the tetracycline antibiotics. The term "tetracycline" is also used to denote the four-ring system of this compound; "tetracyclines" are related substances that contain the same four-ring system.
Antipsychotic agents (1)
This document discusses antipsychotic agents used to treat schizophrenia. It begins with an introduction that explains the positive and negative symptoms of schizophrenia and how antipsychotics work by decreasing dopaminergic neurotransmission. The document then covers the classification of typical and atypical antipsychotics, including examples from different drug classes. It discusses the mechanism of action of phenothiazine derivatives and provides structure-activity relationships. Specific phenothiazine derivatives are highlighted, including chlorpromazine. The document also briefly discusses thioxanthene derivatives as bioisosteres of phenothiazines. In summary, the document provides an overview of antipsychotic agents used to treat schizophrenia, focusing on phenothiazine derivatives and structure-activity relationships
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This document provides an introduction to the pharmacology course taught by Dr. Anubhuti Khare. The goals of the course are to teach students how to safely and effectively prescribe drugs and maintain competency. Educational objectives include describing pharmacokinetics and pharmacodynamics of drugs, indicating appropriate drug use for different diseases while considering cost and safety, and integrating knowledge of addictive drugs and their management. The course also aims to explain pharmacological concepts like prescribing in special medical situations, rational drug therapy, and drug effects during pregnancy and lactation. Assessment methods include short notes, structured essay questions, and identifying drugs according to their uses and adverse effects.
Principles of pharmcology and pharmacotherapeutics
This document provides an overview of key principles of pharmacology. It defines pharmacology and describes its main branches as pharmacodynamics, which examines how drugs act on the body, and pharmacokinetics, which examines what the body does to drugs. Several other branches are also outlined, including pharmacotherapy, chemotherapy, toxicology, clinical pharmacology, and pharmacy. The document concludes by discussing sources of drug information and the nomenclature used for drugs, including their chemical, non-proprietary, and proprietary names.
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Alkaloids
The document discusses alkaloids, which are basic nitrogenous plant compounds that are physiologically active. It defines alkaloids and describes their distribution in plants, forms, nomenclature, extraction and classification. Key points include that alkaloids are found mainly in dicots and families like Apocynaceae, with properties like being crystalline solids, bitter taste, and soluble in organic solvents but not water. Common tests for alkaloids are Mayer's, Dragendorff's, Wagner's and Hager's tests. Alkaloids are classified based on their biogenetic pathway, plant source, basic chemical skeleton or type of amine group.
Nomenclature of optical isomerism
The document discusses the representation and nomenclature of optical isomers. It defines:
- Wedge and dash projection and Fischer projection for representing 3D structures in 2D.
- The D/L and R/S systems for assigning configuration to chiral centers. The D/L system uses hydroxy acid/amino acid and sugar conventions while the R/S system uses Cahn-Ingold-Prelog priority rules.
- Sequence rules for assigning priority to groups around a chiral center in the R/S system.
- Methods for determining R/S configuration including orientation of the lowest priority group and interchanging groups in Fischer projections.
SAR of Morphine
This document discusses structure-activity relationships in drug design and formulation. It introduces Hammett and Hansch plots, which relate reaction rates and biological activity to electronic and physicochemical properties. Modification of lead compounds is explored through changing functional groups, stereochemistry and lipophilicity. Morphine is used as a case study to illustrate how properties like log P, binding groups and stereochemistry impact opioid activity. The conclusion emphasizes the role of medicinal chemistry in understanding disease and developing safer, more effective pharmaceuticals.
Alkaloids
- Alkaloids are basic nitrogen-containing compounds that are often obtained from plants and demonstrate physiological effects.
- They are classified based on their biological origin, biosynthetic pathway, chemical structure, and pharmacological effects.
- Common alkaloids include morphine, quinine, caffeine, and nicotine. They are extracted from plants using various organic solvents and purified.
Medicinal chemistry
This is a ppt on Medicinal chemistry, just made to help out and give the students of CLASS XI studying in CBSE about what Medicinal Chemistry is >>Please do feedback in the comments part
Organized crude drug and unorganized crude drug
This document summarizes organized and unorganized crude drugs. It defines crude drugs as substances obtained from natural sources like plants, animals, and minerals that are used as is without processing except drying and size reduction. Organized crude drugs are obtained from definite anatomic parts of plants like flowers and leaves, have a cellular structure, and are solid. Unorganized crude drugs do not have a cellular structure, can be solid, semisolid or liquid, and are identified through chemical and physical tests rather than microscopic examination. Examples of each type are provided.
Tropane alkaloids notes
This document discusses tropane alkaloids, specifically atropine alkaloid. It summarizes that atropine alkaloid is mainly found in plants from the solanaceae family, like Atropa belladona and Datura stromonium. It then describes the isolation, biosynthesis, identification tests, chemistry and properties, structure-activity relationships, uses, and mechanism of action of atropine alkaloid.
Alkaloids
This document discusses alkaloids, which are nitrogenous plant compounds that have physiological effects. It describes their characteristics, sources, uses, and importance in pharmacy. Key points include: alkaloids are bitter and derived from amino acids; sources include various plant families; uses include analgesic, narcotic, and mydriatic effects; important alkaloids include morphine, codeine, nicotine, and atropine. Tests are outlined to identify the presence of alkaloids. The document also classifies and describes important alkaloid groups such as tropane and solanaceous alkaloids.
Basic metabolic
This document provides an overview of basic metabolic pathways in plants. It discusses primary and secondary metabolism, the role of enzymes and co-enzymes, and several key pathways such as the shikimic acid, acetate, and mevalonate pathways. Primary metabolites such as starch, cellulose, and chlorophyll are synthesized through basic metabolic pathways and are essential for plant growth and function. Secondary metabolites are derived from primary metabolites and have pharmacological activities. Enzymes help catalyze biochemical reactions in metabolic pathways, while co-enzymes assist enzymes and participate in reactions. Biosynthesis converts carbon dioxide into carbohydrates through photosynthesis.
ANTIBIOTICS[PENICILLINS] MEDICINAL CHEMISTRY BY RAVISANKAR
ANTIBIOTICS[PENICILLINS} MEDICIANL CHEMISTRY BY P.RAVISANKAR
VIGNAN PHARMACY COLLEGE
VADLAMUDI
GUNTUR- A.P
INDIA
BIOISOSTERSM
Bioisosterism is a strategy used in drug design that involves replacing one chemical group with another that has similar physical or chemical properties. This is done to improve properties like potency, selectivity, toxicity, and pharmacokinetics without significantly changing the chemical structure. Common bioisosteric replacements include replacing hydrogen with fluorine, replacing carboxylic acids with amides or esters, or replacing phenyl rings with heteroaromatic or saturated rings. The application of bioisosterism has been an important concept in medicinal chemistry for nearly 80 years and will continue to play a role in drug discovery and optimization.
Medicinal chemistry-Anticancer agents
The document discusses various types of anticancer agents, including their classification and mechanisms of action. It focuses on alkylating agents, specifically nitrogen mustards. Nitrogen mustards were some of the first chemicals used to treat cancer and work by alkylating DNA at the N7 position of guanine. This prevents replication and can activate apoptosis. Examples discussed include mechlorethamine, chlorambucil, melphalan, and cyclophosphamide. Cyclophosphamide must be activated in the body to form an aziridinium ion that alkylates DNA. The document also briefly mentions mitomycin C, an antibiotic used in cancer treatment.
Qsar
QSAR attempts to correlate biological activity to measurable physicochemical properties through mathematical equations. It relates parameters like lipophilicity (log P), electronic effects (Hammett constants), and steric effects to biological response. Various QSAR methods exist, including Hansch analysis which uses these substituent constants in its equations. More advanced techniques like CoMFA analyze fields around aligned molecules to model activity landscapes and identify favorable regions for activity. QSAR provides a framework for drug design and predicting activities of untested compounds.
Antimalarial drugs
Natural compounds from the bark of the cinchona tree, most notably quinine was observed to exhibit antimalarial activity.
Until the development of synthetic derivatives (ie. 4-aminoquinoline antimalarials), quinine continued to be the first choice to treat malaria.
Quinine is associated with side effects such as diarrhœa.
4-aminoquinoline antimalarials such as amodiaquine and chloroquine largely replaced quinine because of reduced unpleasant side effects.
The life cycle of the parasite and the immunological defence mechanisms against the parasite are complex.
Part of the parasite’s life cycle involves invasion of red blood cells (erythrocytes).
The haemoglobin within the red blood cell is broken down by the parasite and is used as a source of amino acids.
The 4-aminoquinolines act at the erythrocytic stage of the parasite.
Doxycycline is a compound used in prophylaxis against plasmodial parasites.
Other compounds associated with treating malaria include halofantrine and lumefantrine, often used in combination with other drugs.
Urinary tract anti-infective agent
This document discusses urinary tract infections and various quinolone antibiotics used to treat them. It begins by defining urinary tract infections, distinguishing between lower UTI (cystitis) affecting the bladder and upper UTI (pyelonephritis) affecting the kidneys. Symptoms of lower UTI include pain and frequent urination, while upper UTI additionally causes fever and flank pain. The document then introduces quinolone antibiotics, which are broad-spectrum antibiotics containing a fluoroquinolone. Examples mentioned include ciprofloxacin, levofloxacin, and ofloxacin. The mechanisms of action and classifications of various quinolone generations are briefly outlined. Specific quin
Anticholinergic agent
This document summarizes cholinergic antagonists, which are drugs that block the effects of acetylcholine in the muscarinic receptor. It discusses their structure-activity relationships, medical uses in conditions like ulcers, overactive bladder, and organophosphate poisoning. Specific antagonists are described like atropine, hyoscyamine, scopolamine, ipratropium, tiotropium, benztropine, biperiden, tropicamide, and others. Their mechanisms of action, pharmacological effects, and clinical applications are concisely outlined.
Definition, historical landmarks, scope of pharmacology
This presentation highlights Definition, historical landmarks & scope of pharmacology. It also includes essential medicines.
Alkaloids Pharmacognosy
The document provides information about a presentation on alkaloids. It discusses that alkaloids are basic nitrogen-containing compounds found mainly in plants. They have a complex molecular structure and show significant pharmacological activity. Alkaloids are classified based on whether the nitrogen is part of a ring or not. They exhibit diverse physical and chemical properties and are tested using various chemical reagents like Mayer's reagent. Alkaloids have many uses as analgesics, antihypertensives, and in treating other medical conditions due to their pharmacological activities. Examples of alkaloid-containing plants discussed include Lobelia, which has expectorant properties.
Tetracycline sar
-a broad-spectrum antibiotics.
-It is commonly used to treat acne, infection, and other infections caused by bacteria.
-The first of these compounds was chlortetracycline followed by oxytetracycline and tetracycline.
Tetracycline is a broad-spectrum polyketide antibiotic produced by the Streptomyces genus of Actinobacteria, indicated for use against many bacterial infections. It is a protein synthesis inhibitor. It is commonly used to treat acne today, and, more recently, rosacea, and is historically important in reducing the number of deaths from cholera. Tetracycline is marketed under the brand names Sumycin, Tetracyn, and Panmycin, among others. Actisite is a thread-like fiber formulation used in dental applications. It is also used to produce several semisynthetic derivatives, which together are known as the tetracycline antibiotics. The term "tetracycline" is also used to denote the four-ring system of this compound; "tetracyclines" are related substances that contain the same four-ring system.
Antipsychotic agents (1)
This document discusses antipsychotic agents used to treat schizophrenia. It begins with an introduction that explains the positive and negative symptoms of schizophrenia and how antipsychotics work by decreasing dopaminergic neurotransmission. The document then covers the classification of typical and atypical antipsychotics, including examples from different drug classes. It discusses the mechanism of action of phenothiazine derivatives and provides structure-activity relationships. Specific phenothiazine derivatives are highlighted, including chlorpromazine. The document also briefly discusses thioxanthene derivatives as bioisosteres of phenothiazines. In summary, the document provides an overview of antipsychotic agents used to treat schizophrenia, focusing on phenothiazine derivatives and structure-activity relationships
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ANTIBIOTICS[PENICILLINS] MEDICINAL CHEMISTRY BY RAVISANKAR
ANTIBIOTICS[PENICILLINS] MEDICINAL CHEMISTRY BY RAVISANKAR
Definition, historical landmarks, scope of pharmacology
Definition, historical landmarks, scope of pharmacology
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2. Pharmacokinetics studies what the body does to drugs through absorption, distribution, metabolism, and excretion. Pharmacodynamics examines a drug's molecular, biochemical, and physiological effects.
3. Safety testing of drugs includes assessing adverse drug reactions through clinical trials and pharmacovigilance programs.
Introduction to pharmacology
This document contains a syllabus and objectives for a pharmacology course. The syllabus covers topics like general pharmacology, drugs acting on different body systems like the ANS, CVS, CNS, and drugs for blood, diabetes, respiratory system etc. It lists 5 textbooks used for the course. The objectives section defines key terms like pharmacology, drug, and branches of pharmacology. It explains why pharmacology is important for treating disease and lists the main therapeutic methods. It also provides examples of natural sources of drugs and the nature and categories of drugs. The document assigns a homework on the sources and nature of drugs.
Introduction Medication Administration
This document defines key terms and concepts in pharmacology. It discusses how pharmacology is the study of drug interactions with living systems. The four main processes that determine a drug's effects are absorption, distribution, metabolism, and excretion. Factors like genetics, age, and health conditions can influence how individuals respond to drugs. Adverse reactions, drug interactions, and tolerance are important considerations when using medications. Standards and regulations aim to ensure drugs are safe, effective, and produced consistently.
general pharma.pptx
1.1 Pharmacology- An Introduction
The word pharmacology is derived from two Greek words, pharmacon meaning a drug, and logos meaning an opinion or reason. It can be defined as
“The science which deals with the history, source, physical properties, chemical properties, compounding, biochemical effects, physiological effects, mechanism of action, absorption, distribution, biotransformation, excretion, therapeutic and other uses of drugs, is called pharmacology.”
“The study of a substance that interacts with the living system through chemical processes especially by binding to regulatory molecules and activates or inhibits normal body processes”
“The science of substances used to prevent, diagnose and treat disease.”
Drug:
The word drug comes from Drogue meaning a dry herb. A drug can be defined as:
“A substance, material or product used for the purpose of diagnosis, prevention and relief of symptoms or cure of disease.”
WHO defines drug as:
“A substance, material or product used or intended to be used to modify or explore the physiological processes or pathological states for the benefit of the recipient.”
General Features of a Drug:
• Variability in molecular size
• Variability in shape
• Variability in chemical nature
• Variability in lipid/water partition coefficient
• Variability in degree of ionization
• Physical Properties
• Variability in molecular size
Smaller sized molecules are easily absorbed than larger molecules. Normally the molecular weight is between 100-1000 but may be higher or lower. Streptokinase is an example of large molecular weight drug while lithium or nitric oxides are of small molecular weight.
• Variability in shape
Pharmacology
This document provides an overview of pharmacology. It defines pharmacology and its main divisions of pharmacodynamics and pharmacokinetics. It discusses the history of pharmacology and covers essential aspects like routes of drug administration, essential drug concepts, drug nomenclature, and classifications of prescribed vs non-prescribed drugs. The summary briefly outlines what pharmacology is, its main divisions and aspects covered in the document like routes of administration and drug classifications.
Scope of Pharmacology
Pharmacology and toxicology are the study of the effects of drugs and chemicals on living organisms. A toxicologist examines how substances cause adverse health effects on humans, animals and the environment. The history of pharmacology involved early experimentation with animals to determine drug actions. Toxicologists work in various areas including mechanistic toxicology to understand disease mechanisms, descriptive toxicology for toxicity testing, regulatory toxicology for rulemaking, and translational toxicology applying basic research to patients. Their work assesses chemical risks and ensures product and environmental safety.
opcional medicinal-desbloqueado.pdf
This document discusses various topics related to pharmaceutical products and drug action:
- Medicines and drugs have different effects on the body and can alter sensations, mood, physiological states, and activity levels. They are classified into categories like depressants, stimulants, and hallucinogens.
- Natural products from plants are chemically extracted and modified to produce more potent and safer medicines, some of which can become addictive substances of abuse if misused.
- Drugs are classified differently between countries and may require a prescription, be available over-the-counter, or be illegal depending on their potential for abuse and medical usefulness. Their classification and availability is regulated to help ensure safety.
Introduction to Pharmacol.pdf
This document provides an introduction to pharmacology. It defines key terms like pharmacology, pharmacodynamics, pharmacokinetics, and discusses the history and divisions of pharmacology. It also covers drug nomenclature, essential medicines, orphan drugs, and provides definitions of related terms like pharmacy, pharmaceutics, and toxicology. The document is presented by Prof. Shaikh Abusufiyan and aims to explain fundamental concepts in pharmacology to students.
Medicinal chemistry unit1&3
This document provides an overview of the field of medicinal chemistry. It defines medicinal chemistry as an interdisciplinary research area that incorporates different branches of chemistry and biology to research and develop new drugs. The roles of medicinal chemists include synthesizing and characterizing new compounds, determining biological effects, optimizing lead compounds, and studying pharmacokinetic properties. It also discusses the drug development process and clinical trials. Key aspects covered include drug classification, sources of drug leads, and factors that influence drug properties such as stability and bioavailability.
_1_Intro_to_OrgMed.ppt.pptx
Medicinal chemistry is the science of discovering and designing new drugs. It is an interdisciplinary field that uses principles of chemistry and biology. The goals of medicinal chemistry are to make new compounds, study how compounds affect biological processes, and alter compound structures to optimize effects and reduce side effects. Medicinal chemists work to discover, develop, and optimize drug candidates through a process involving lead discovery, lead optimization, and clinical trials.
GENERAL PHARMACOLOGY.pptx
Pharmacology is the study of how drugs interact with living organisms. Key aspects include examining drug actions and effects, how drugs are absorbed and metabolized by the body, and relationships between drug concentrations and biological responses. Drugs come from natural sources like plants, animals, and microorganisms, as well as through synthetic chemistry and biotechnology. Routes of administration impact drug onset times and effectiveness.
Introduction to pharmacology 2018 updated
This document provides an introduction to the key concepts in pharmacology. It discusses what pharmacology is, the rational use of drugs, and drug characteristics such as sources, classification, and names. It outlines major drug uses in clinical practice and general principles of rational drug prescribing. Key points covered include drug classification systems based on therapeutic use and pharmacologic mechanisms. Adverse drug effects and their specific forms are examined. Pregnancy categories and drug nomenclature are also summarized. The overall objectives of pharmacology and drug therapy are to provide maximum benefit and efficacy while minimizing harm and toxicity.
01.0 introduction to cp course
This document provides an introduction to a clinical pharmacology course. It discusses the expectations for students in the course, challenges doctors may face with prescribing drugs, and a brief history of pharmacology as a scientific discipline. The challenges include an increasing number of drugs, more complex patient treatment regimens, and potential threats from the pharmaceutical industry. The history overview describes how pharmacology emerged alongside advances in chemistry, physiology and the cell theory. It also discusses alternative therapeutic approaches compared to modern evidence-based medicine.
01.0 introduction to cp course copy
This document provides an introduction to a clinical pharmacology course. It discusses the challenges doctors face with an increasing number of drugs and complex patient treatment regimens. It outlines the course objectives to produce competent prescribers and provide a framework for assimilating new drug information. The document also reviews the history and development of pharmacology as a scientific discipline and contrasts modern medicine's reliance on drugs compared to alternative therapeutic principles.
An Introduction to Pharmacology
This document provides an introduction to the Department of Pharmacology at NEIGRIHMS. It discusses the history of pharmacology and some pioneering figures. Pharmacology is defined as the study of how chemicals affect living processes, including drugs, hormones, neurotransmitters and toxic agents. The roles of pharmacologists and medicinal chemists in drug discovery are described. Key terms like drug, pharmacokinetics, pharmacodynamics and therapeutic agents are defined. The relationships between pharmacokinetics and pharmacodynamics are outlined. Recommended pharmacology textbooks are also listed.
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Ch1 introduction to medicinal chemistry
- 1. MEDICINAL CHEMISTRY I BY AKLILU 1
- 3. CHAPTER ONE: INTRODUCTION Definition and its relation to other disciplines Source and classification of drugs Nomenclature of drugs 3
- 4. Definition: • It is chemistry-based discipline, also involving aspects of biological, medical and pharmaceutical sciences. • It is applied science that is focused on the design (or discovery) of new chemical entities (NCEs) and their optimization and development as useful drug molecules for the treatment of disease processes”. 4
- 5. Definition: • Structure-activity relationship (SAR) is the relationship between chemical structure and pharmacological activity for a series of compounds. 5 It is concerned with o the invention, discovery, design, identification and preparation of biologically active compounds, o the study of their metabolism, the interpretation of their mode of action at the molecular level and o the construction of structure-activity relationships (SAR).
- 6. Definition: • Medicinal chemistry covers three critical steps: 6 Discover step Optimization step Development stage
- 7. 7 Discover step • Involving choice of therapeutic target (receptor, enzyme& target group) • Identification and production of new active substances interacting with selected targets. • Such compounds called LEADCOMPOUND. Optimization step • Which deals with improvement of lead compound • The optimization process takes primarily into account the increase in potency, selectivity Development stage Whose purpose is continuation of improvement of pharmacokinetic properties
- 8. 8 Reading assignment Origin of medicinal chemistry
- 9. Relation to other disciplines • Medicinal chemistry is disciplines at the intersection of chemistry, especially synthetic organic chemistry, and pharmacology and various other biological specialties, Biochemistry, Molecular biology. 9
- 10. Relation to other disciplines • It relate to 10 Chemistry Medicinal chemistry
- 11. Source and classification of drugs What are drugs? • Drugs are chemical substances that are used to prevent or treat diseases in humans, animals and plants. • They may also be used for making a medical diagnosis or for restoring, correcting, or modifying physiological functions. 11
- 12. What are drugs? • Drugs can act as poisons if taken in excess. • overdoses of paracetamol can cause coma and death. • In addition to their beneficial effects, most drugs have non-beneficial biological effects. • Aspirin, which is commonly used to alleviate headaches, may also cause gastric irritation and bleeding. • These unwanted effects are commonly referred to as side effects. 12
- 13. Natural Sources of drugs • Generally sources of drugs are 13 Plants Animals Synthetic Semi synthetic
- 14. Classification of drugs There is no homogeneous system for classifying drugs Drugs are classified in a number of different ways depending on where and how the drugs are being used. • Chemical structures • Pharmacological Action • Drugs can treat different types of diseases 14
- 15. 1. Chemical structures: alkaloids, steroids, glycosides, etc 15
- 16. 2. Pharmacological Action: • Site of action: Cellular site e.g., loop diuretic, catecholamine uptake inhibitor • Body system e.g. cardiovascular, alimentary 16
- 17. 3. Drugs can treat different types of diseases: • 1-Infectious diseases: Born (transmitted) from person to person by outside agents, bacteria (pneumonia, salmonella), viruses (common cold, AIDS), fungi (thrush, athletes foot), parasites (malaria) • 2-Non-infectious diseases: disorders of the human body caused by genetic malfunction, environmental factors, stress, old age etc. (e.g. diabetes, heart disease, cancer. Haemophilia, asthma, mental illness, stomach ulcers, arthritis). • 3-Non-diseases: alleviation of pain (analgesic), prevention of pregnancy (contraception) , anesthesia. 17
- 18. Nomenclature of drugs • There are basically three classes of drug names which is recognized by drug companies and regulatory bodies 18 Chemical names Generic/Non-proprietary /Approved names Trade/Brand names /Proprietary
- 19. 1. Chemical names • Are the scientific (IUPAC) names, based on the molecular structure of the drug. • Are useful for chemists or technical personnel • Not suitable for common use in prescribing drugs 19 Paracetamol N-(4-hydroxyphenyl)-acetamide
- 20. 2. Generic names • They are official names assigned by national regulatory agencies • It avoids the confusion of giving several names to the same drug Example • Co-trimoxazole, Diclofenac, Omeprazole, Paracetamol 20
- 21. 3. Trade/Brand names • Names given to the drug by the manufacturing and marketing company • In most cases one drug could have so many (multiple) trade/brand names 21 Acetaminophen has many trade names such as • Paracetamol • Tylenol • Paramol • Panadol • cadimol • Capol etc.
- 22. 22 Thank you for watching Join blu pharmacy on telegram for more books and ppt https://t.me/pharmacyRxx Facebook Log in or sign up to send message https://www.facebook.com/akyeako