Once a lead compound or a pharmacophore structure with the desired pharmacological effect has been identified, organic chemists can introduce modifications in the chemical structure of the lead compound with the goal of improving the pharmacokinetics or pharmacodynamics of a drug candidate. These evolved structures are known as analogs.
3
stereochemistry and drug action ; basic introduction about stereochemistry and stereoisomers ; pharmacokinetic and pharmacodynamics concept of stereochemistry ; easson Stedman hypothesis ; stereo selectivity criteria .
Introduction
Classification
Therapeutic values of peptidomimetics
Design of peptidomimetics by manipulation of amino acids
Modification of peptide backbone
Chemistry of prostaglandins, leukotrienes and thromboxanes
This powerpoint presentation will help to know about introduction of bioisosterism by Biotechnology point of view. Hope this powerpoint presentation will your reference.
stereochemistry and drug action ; basic introduction about stereochemistry and stereoisomers ; pharmacokinetic and pharmacodynamics concept of stereochemistry ; easson Stedman hypothesis ; stereo selectivity criteria .
Introduction
Classification
Therapeutic values of peptidomimetics
Design of peptidomimetics by manipulation of amino acids
Modification of peptide backbone
Chemistry of prostaglandins, leukotrienes and thromboxanes
This powerpoint presentation will help to know about introduction of bioisosterism by Biotechnology point of view. Hope this powerpoint presentation will your reference.
PEPTIDOMIMETICS , HERE WE HAVE INCLUDED THE INTRODUCTION, CLASSIFICATION, ADVANTAGES , DISADVANTAGES, ITS METHODS PREPARATION, PRINCIPLES OD DRUG DESIGN, ITS CHEMISTRY. STEREOCHEMISTRY, SYNTHESIS AND APPLICATIONS
Peptidomimetics are compounds whose essential elements (pharmacophore) mimic a natural peptide or protein in 3D space and which retain the ability to interact with the biological target and produce the same biological effect.
Peptidomimetics are designed to circumvent some of the problems associated with a natural peptide for example
Stability against proteolysis (duration of activity)
Poor bioavailability.
Receptor selectivity or potency (often can be substantially improved).
The Hammett Plot is a type of Linear Free-Energy Relationship (LFER) analysis designed to model the electronic effect of substituents on aromatic systems (in the para and meta positions only). Information gathered can be used to probe the mechanism of the reaction and can be applied in the optimization of reaction conditions.
Contributed by: Eric Amerling & Christine Nervig (Undergraduates), University of Utah, 2013
Stereochemistry is the ‘chemistry of space’ , that is stereochemistry deals with the spatial arrangements of atoms and groups in a molecule.
Stereochemistry can trace its roots to the year 1842 when the French chemist Louis Pasteur made an observation that the salts of tartaric acid collected from a wine production vessel have the ability to rotate plane-polarized light, whereas the same salts from different sources did not have this ability.
Isomers are compounds that contain exactly the same number of atoms, i.e., they have exactly the same empirical formula, but differ from each other by the way in which the atoms are arranged.
Constitutional isomers, also known as structural isomers, are specific types of isomers that share the same molecular formula but have different bonding atomic organization and bonding patterns.
Stereoisomers are molecules having the same molecular formula and the atomic arrangement, but differ in their spatial arrangement.
Geometric isomers are two or more coordination compounds which contain the same number and types of atoms, and bonds (i.e., the connectivity between atoms is the same), but which have different spatial arrangements of the atoms.
There are 2 types of geometric isomers, ‘cis’ and ‘trans’. -cis isomers: when similar groups are present on the same side of the double bonds, then they are termed as cis. - trans isomers: when similar groups are present on the opposite sides of the double bonds then they are called trans isomers.
cis-diethylstilbestrol has only 7% of the estrogenic activity of trans-diethylstilbesterol.
Cisplatin have anticancer activity where ae trans platin is an inactive compound.
In chemistry, a molecule or ion is called chiral if it cannot be superposed on its mirror image by any combination of rotations, translations, and some conformational changes.
Chirality is the property of being non identical to ones mirror image.
Chiral center is defined as the atom bearing 4 different atoms or group of atoms.
Molecules that form nonsuperimposable mirror images, and thus exist as enantiomers, are said to be chiral molecules.
For a molecule to be chiral, it cannot contain a plane of symmetry.
The term enantioselectivity refers to the efficiency with which the reaction produces one enantiomer.
Enantiomers are stereoisomers that are non-superimposable mirror images.
Have identical properties.
Similar shapes
Diastereomers are stereoisomers that are non superimposable and are not mirror images.
Have distinct physical properties.
Have different molecular shapes.
Enantiomers consist of a pair of molecules that are mirror images of each other and are not superimposable.
When a molecule contains only one chiral centre , the two stereoisomers are known as enantiomers.
These may be referred to or labelled using the configurational descriptors as either:
R(rectus meaning right handed) or S(sinister meaning left handed),
D(dextrorotatory)or L (laevorotatory)
E-Entgegen or Z- Zusamen
more chemistry contents are available
1. pdf file on Termmate: https://www.termmate.com/rabia.aziz
2. YouTube: https://www.youtube.com/channel/UCKxWnNdskGHnZFS0h1QRTEA
3. Facebook: https://web.facebook.com/Chemist.Rabia.Aziz/
4. Blogger: https://chemistry-academy.blogspot.com/
Organic Synthesis:
The Disconnection Approach
One Group C-C Disconnection of Alcohol and Alkene
THE SOLID PHASE PEPTIDE SYNTHESIS IS SLIGHTLY DIFFRENT FROM PEPTIDE SYNTHESIS WHICH IS DISCUSSED HERE, ITS SYNTHESIS WITH STRUCTURE ANS BASICS ARE DISCUSSED WHICH WILL BE VERY USEFUL FOR READERS.
PEPTIDOMIMETICS , HERE WE HAVE INCLUDED THE INTRODUCTION, CLASSIFICATION, ADVANTAGES , DISADVANTAGES, ITS METHODS PREPARATION, PRINCIPLES OD DRUG DESIGN, ITS CHEMISTRY. STEREOCHEMISTRY, SYNTHESIS AND APPLICATIONS
Peptidomimetics are compounds whose essential elements (pharmacophore) mimic a natural peptide or protein in 3D space and which retain the ability to interact with the biological target and produce the same biological effect.
Peptidomimetics are designed to circumvent some of the problems associated with a natural peptide for example
Stability against proteolysis (duration of activity)
Poor bioavailability.
Receptor selectivity or potency (often can be substantially improved).
The Hammett Plot is a type of Linear Free-Energy Relationship (LFER) analysis designed to model the electronic effect of substituents on aromatic systems (in the para and meta positions only). Information gathered can be used to probe the mechanism of the reaction and can be applied in the optimization of reaction conditions.
Contributed by: Eric Amerling & Christine Nervig (Undergraduates), University of Utah, 2013
Stereochemistry is the ‘chemistry of space’ , that is stereochemistry deals with the spatial arrangements of atoms and groups in a molecule.
Stereochemistry can trace its roots to the year 1842 when the French chemist Louis Pasteur made an observation that the salts of tartaric acid collected from a wine production vessel have the ability to rotate plane-polarized light, whereas the same salts from different sources did not have this ability.
Isomers are compounds that contain exactly the same number of atoms, i.e., they have exactly the same empirical formula, but differ from each other by the way in which the atoms are arranged.
Constitutional isomers, also known as structural isomers, are specific types of isomers that share the same molecular formula but have different bonding atomic organization and bonding patterns.
Stereoisomers are molecules having the same molecular formula and the atomic arrangement, but differ in their spatial arrangement.
Geometric isomers are two or more coordination compounds which contain the same number and types of atoms, and bonds (i.e., the connectivity between atoms is the same), but which have different spatial arrangements of the atoms.
There are 2 types of geometric isomers, ‘cis’ and ‘trans’. -cis isomers: when similar groups are present on the same side of the double bonds, then they are termed as cis. - trans isomers: when similar groups are present on the opposite sides of the double bonds then they are called trans isomers.
cis-diethylstilbestrol has only 7% of the estrogenic activity of trans-diethylstilbesterol.
Cisplatin have anticancer activity where ae trans platin is an inactive compound.
In chemistry, a molecule or ion is called chiral if it cannot be superposed on its mirror image by any combination of rotations, translations, and some conformational changes.
Chirality is the property of being non identical to ones mirror image.
Chiral center is defined as the atom bearing 4 different atoms or group of atoms.
Molecules that form nonsuperimposable mirror images, and thus exist as enantiomers, are said to be chiral molecules.
For a molecule to be chiral, it cannot contain a plane of symmetry.
The term enantioselectivity refers to the efficiency with which the reaction produces one enantiomer.
Enantiomers are stereoisomers that are non-superimposable mirror images.
Have identical properties.
Similar shapes
Diastereomers are stereoisomers that are non superimposable and are not mirror images.
Have distinct physical properties.
Have different molecular shapes.
Enantiomers consist of a pair of molecules that are mirror images of each other and are not superimposable.
When a molecule contains only one chiral centre , the two stereoisomers are known as enantiomers.
These may be referred to or labelled using the configurational descriptors as either:
R(rectus meaning right handed) or S(sinister meaning left handed),
D(dextrorotatory)or L (laevorotatory)
E-Entgegen or Z- Zusamen
more chemistry contents are available
1. pdf file on Termmate: https://www.termmate.com/rabia.aziz
2. YouTube: https://www.youtube.com/channel/UCKxWnNdskGHnZFS0h1QRTEA
3. Facebook: https://web.facebook.com/Chemist.Rabia.Aziz/
4. Blogger: https://chemistry-academy.blogspot.com/
Organic Synthesis:
The Disconnection Approach
One Group C-C Disconnection of Alcohol and Alkene
THE SOLID PHASE PEPTIDE SYNTHESIS IS SLIGHTLY DIFFRENT FROM PEPTIDE SYNTHESIS WHICH IS DISCUSSED HERE, ITS SYNTHESIS WITH STRUCTURE ANS BASICS ARE DISCUSSED WHICH WILL BE VERY USEFUL FOR READERS.
DRUG DISCOVERY
Drug Discovery without a lead
LEAD DISCOVERY/IDENTIFICATION
LEAD MODIFICATION
CONCEPT OF PRODRUGS AND SOFT DRUGS
DRUG RECEPTOR INTERACTIONS
Drug-Drug interactions (DDI) is a serious clinical issue. An important mechanism underlying of DDI, is
induction or inhibition of drug metabolizing enzymes (DMEs) and transporters that mediate metabolism, cellular uptake and efflux of xenobiotics. DDI cannot be avoided in many cases, as they belong to routine medical practice.
THE PRODRUG DESIGNING FOR NEW SELECTION AND FORMULATION OF DRUG COMPATIBLE WITH API I.E. ACTIVE PHARMACUTICAL INGREDIENT, AND ITS EFFECT WHICH SHOULD BE 0. THE DRUG COMBINED WITH API AND AVILABLE IN MARKET AND DRUGS NEED TO BE COMBINE ARE ALSO DISCUSSED WITH ITS STRUCTURE AND SAR, AND COVERED AS PER THE SYLLABUS OF PCI.
Introduction of Veterinary pharmacologyQaline Giigii
this course of Introduction of veterinary pharacology was presented by Dr. Osman Abdulahi Farah
Osman Shiine
at Gollis University faculty of Veterinary Medicine
2014
Introduction of Veterinary pharmacology Somaliland Dr.Osman Abdulahi FarahQaline Giigii
This course was prepared by Dr.Osman Abdulahi Farah
Cismaan shiine Lecturer of Gollis University Faculty of Agriculture and Veterinary Medicine 2014
The main content of this course including introduction of Veterinary Pharmacology, division of pharmacology and list of terms of terminology about veterinay pharmacology
In 1891,Emil fischer devised a method of representing the 3D structures of
molecules in 2D Structures on a plane (Paper) by convention, horizontal line
represent bonds projecting from the plane of paper towards the observer and
vertical line represent away from the observer
Flash photolysis and Shock tube method PRUTHVIRAJ K
In 1967 the Nobel prize in chemistry was awarded to Manfred Eigen, Ronald George Wreyford Norrish for their co-discovery of Flash photolysis in 1949.
Flash photolysis is used to extensively to study reactions that happen extremely quickly, even down to the femtosecond depending on the laser that is used. The technique was born out of cameras developed during and shorty after WWII, which were used to take pictures of fast moving planes, rockets and Missiles.
Since then the technology of laser and optics has progressed allowing faster and faster reactions to be studied.
A silicate is an anions consisting of silicon and oxygen.
Silicates occur in earth’s crust in abundantly in the form of silicate minerals and aluminosilicate clay.
Silicate anions are often large polymeric molecules with an extense variety of structures,including chains and rings.double chains and sheets.
Silicates are extremely important materials, both natural and artificial, for all sorts of technological and artistic activities.
IDENTIFICATION OF ACTIVE PART : THE PHARMACOPHOREPRUTHVIRAJ K
Portion of the molecule containing the essential organic functional groups that directly interact with the receptor active site and are responsible for the activity are know as pharmacophore.
Pharmacophore model represents the binding mode of active molecules to their target.
A pharmacophore model differentiates between active and inactive molecule.
STRUCTURE MODIFICATION TO INCREASE POTENCY AND THERAPEUTIC INDEX PRUTHVIRAJ K
1. It is a tool of research in medicinal chemistry to refine molecule.
2.Most of the molecules are modified either by altering its physical properties or by modifying chemical structure.
Structure modification is chemical alteration of known and previously characterized.
lead compound for the purpose of enhancing its usefulness as a drug (to improve activity).
This could mean enhancing its specificity for a particular body target site, increasing its potency.
Examples:
Progesterone and estradiol among the sex hormones
Nucleophilic Substitution reaction (SN1 reaction)PRUTHVIRAJ K
Attack of nucleophile at a saturated carbon atom bearing substituent, known as leaving group results in Substitution reaction.
The group that is displaced (leaving group) carries its bonding electrons.
The new bond is formed between nucleophile and the carbon using the electrons supplied by the nucleophilic agent.
The compound on which substitution takes place is called “substrate.”
The substrate consists of two parts, alkyl group and leaving group.
UNIMOLECULAR SURFACE REACTION: MECHANISM, INHIBITION AND ACTIVATION ENERGYPRUTHVIRAJ K
Unimolecular surface reaction may involve a reaction between a molecule A of the reactant and vacant site S on the surface
Surface reaction involving single adsorbed molecules and therefore term as unimolecular and are treated by Langmuir adsorption isotherm
Kinetics of Pyrolysis of acetaldehyde PRUTHVIRAJ K
Pyrolysis is a chain reaction process in which the compound is converted into smaller fragments in the absence of oxygen
this content explains kinetics of primary splitting of acetaldehyde molecule to form methyl radicals and further decomposition leads to the formation of hydrogen.
Diel's-Alder and Gattermann Koch ReactionsPRUTHVIRAJ K
n organic chemistry, the Diels–Alder reaction is a chemical reaction between a conjugated diene and a substituted alkene, commonly termed the dienophile, to form a substituted cyclohexene derivative. It is the prototypical example of a pericyclic reaction with a concerted mechanism
The Chichibabin reaction is a method for producing 2-aminopyridine derivatives by the reaction of pyridine with sodium amide. It was reported by Aleksei Chichibabin in 1914. The following is the overall form of the general reaction: The direct amination of pyridine with sodium amide takes place in liquid ammonia
The benzoin addition is an addition reaction involving two aldehydes. The reaction generally occurs between aromatic aldehydes or glyoxals. The reaction produces an acyloin. In the classic application benzaldehyde is converted to benzoin
Pigments and Colors: Natural Pigments or Plant Pigments PRUTHVIRAJ K
Biological pigments, also known simply as pigments or biochromes, are substances produced by living organisms that have a color resulting from selective color absorption. Biological pigments include plant pigments and flower pigment
A pigment is a colored material that is completely or nearly insoluble in water. In contrast, dyes are typically soluble, at least at some stage in their use. Generally, dyes(Colors) are often organic compounds whereas pigments are often inorganic compounds
The Cannizzaro reaction, named after its discoverer Stanislao Cannizzaro, is a chemical reaction that involves the base-induced disproportionation of two molecules of a non-enolizable aldehyde to give a primary alcohol and a carboxylic acid
Conformational analysis of medium ringsPRUTHVIRAJ K
Conformational analysis of medium rings: Spatial arrangement and conformation of 7membered, 8membered, 9 and 10membered rings, nature of hydrogen and carbon atoms
Pigments and Colors:Extraction and PurificationPRUTHVIRAJ K
Pigments and Colors:Extraction and Purification- Extraction of naturally occurring pigments like anthocyanins, tannins etc from their sources and purification methods
Synthetic Fiber Construction in lab .pptxPavel ( NSTU)
Synthetic fiber production is a fascinating and complex field that blends chemistry, engineering, and environmental science. By understanding these aspects, students can gain a comprehensive view of synthetic fiber production, its impact on society and the environment, and the potential for future innovations. Synthetic fibers play a crucial role in modern society, impacting various aspects of daily life, industry, and the environment. ynthetic fibers are integral to modern life, offering a range of benefits from cost-effectiveness and versatility to innovative applications and performance characteristics. While they pose environmental challenges, ongoing research and development aim to create more sustainable and eco-friendly alternatives. Understanding the importance of synthetic fibers helps in appreciating their role in the economy, industry, and daily life, while also emphasizing the need for sustainable practices and innovation.
Embracing GenAI - A Strategic ImperativePeter Windle
Artificial Intelligence (AI) technologies such as Generative AI, Image Generators and Large Language Models have had a dramatic impact on teaching, learning and assessment over the past 18 months. The most immediate threat AI posed was to Academic Integrity with Higher Education Institutes (HEIs) focusing their efforts on combating the use of GenAI in assessment. Guidelines were developed for staff and students, policies put in place too. Innovative educators have forged paths in the use of Generative AI for teaching, learning and assessments leading to pockets of transformation springing up across HEIs, often with little or no top-down guidance, support or direction.
This Gasta posits a strategic approach to integrating AI into HEIs to prepare staff, students and the curriculum for an evolving world and workplace. We will highlight the advantages of working with these technologies beyond the realm of teaching, learning and assessment by considering prompt engineering skills, industry impact, curriculum changes, and the need for staff upskilling. In contrast, not engaging strategically with Generative AI poses risks, including falling behind peers, missed opportunities and failing to ensure our graduates remain employable. The rapid evolution of AI technologies necessitates a proactive and strategic approach if we are to remain relevant.
Introduction to AI for Nonprofits with Tapp NetworkTechSoup
Dive into the world of AI! Experts Jon Hill and Tareq Monaur will guide you through AI's role in enhancing nonprofit websites and basic marketing strategies, making it easy to understand and apply.
How to Make a Field invisible in Odoo 17Celine George
It is possible to hide or invisible some fields in odoo. Commonly using “invisible” attribute in the field definition to invisible the fields. This slide will show how to make a field invisible in odoo 17.
June 3, 2024 Anti-Semitism Letter Sent to MIT President Kornbluth and MIT Cor...Levi Shapiro
Letter from the Congress of the United States regarding Anti-Semitism sent June 3rd to MIT President Sally Kornbluth, MIT Corp Chair, Mark Gorenberg
Dear Dr. Kornbluth and Mr. Gorenberg,
The US House of Representatives is deeply concerned by ongoing and pervasive acts of antisemitic
harassment and intimidation at the Massachusetts Institute of Technology (MIT). Failing to act decisively to ensure a safe learning environment for all students would be a grave dereliction of your responsibilities as President of MIT and Chair of the MIT Corporation.
This Congress will not stand idly by and allow an environment hostile to Jewish students to persist. The House believes that your institution is in violation of Title VI of the Civil Rights Act, and the inability or
unwillingness to rectify this violation through action requires accountability.
Postsecondary education is a unique opportunity for students to learn and have their ideas and beliefs challenged. However, universities receiving hundreds of millions of federal funds annually have denied
students that opportunity and have been hijacked to become venues for the promotion of terrorism, antisemitic harassment and intimidation, unlawful encampments, and in some cases, assaults and riots.
The House of Representatives will not countenance the use of federal funds to indoctrinate students into hateful, antisemitic, anti-American supporters of terrorism. Investigations into campus antisemitism by the Committee on Education and the Workforce and the Committee on Ways and Means have been expanded into a Congress-wide probe across all relevant jurisdictions to address this national crisis. The undersigned Committees will conduct oversight into the use of federal funds at MIT and its learning environment under authorities granted to each Committee.
• The Committee on Education and the Workforce has been investigating your institution since December 7, 2023. The Committee has broad jurisdiction over postsecondary education, including its compliance with Title VI of the Civil Rights Act, campus safety concerns over disruptions to the learning environment, and the awarding of federal student aid under the Higher Education Act.
• The Committee on Oversight and Accountability is investigating the sources of funding and other support flowing to groups espousing pro-Hamas propaganda and engaged in antisemitic harassment and intimidation of students. The Committee on Oversight and Accountability is the principal oversight committee of the US House of Representatives and has broad authority to investigate “any matter” at “any time” under House Rule X.
• The Committee on Ways and Means has been investigating several universities since November 15, 2023, when the Committee held a hearing entitled From Ivory Towers to Dark Corners: Investigating the Nexus Between Antisemitism, Tax-Exempt Universities, and Terror Financing. The Committee followed the hearing with letters to those institutions on January 10, 202
The Roman Empire A Historical Colossus.pdfkaushalkr1407
The Roman Empire, a vast and enduring power, stands as one of history's most remarkable civilizations, leaving an indelible imprint on the world. It emerged from the Roman Republic, transitioning into an imperial powerhouse under the leadership of Augustus Caesar in 27 BCE. This transformation marked the beginning of an era defined by unprecedented territorial expansion, architectural marvels, and profound cultural influence.
The empire's roots lie in the city of Rome, founded, according to legend, by Romulus in 753 BCE. Over centuries, Rome evolved from a small settlement to a formidable republic, characterized by a complex political system with elected officials and checks on power. However, internal strife, class conflicts, and military ambitions paved the way for the end of the Republic. Julius Caesar’s dictatorship and subsequent assassination in 44 BCE created a power vacuum, leading to a civil war. Octavian, later Augustus, emerged victorious, heralding the Roman Empire’s birth.
Under Augustus, the empire experienced the Pax Romana, a 200-year period of relative peace and stability. Augustus reformed the military, established efficient administrative systems, and initiated grand construction projects. The empire's borders expanded, encompassing territories from Britain to Egypt and from Spain to the Euphrates. Roman legions, renowned for their discipline and engineering prowess, secured and maintained these vast territories, building roads, fortifications, and cities that facilitated control and integration.
The Roman Empire’s society was hierarchical, with a rigid class system. At the top were the patricians, wealthy elites who held significant political power. Below them were the plebeians, free citizens with limited political influence, and the vast numbers of slaves who formed the backbone of the economy. The family unit was central, governed by the paterfamilias, the male head who held absolute authority.
Culturally, the Romans were eclectic, absorbing and adapting elements from the civilizations they encountered, particularly the Greeks. Roman art, literature, and philosophy reflected this synthesis, creating a rich cultural tapestry. Latin, the Roman language, became the lingua franca of the Western world, influencing numerous modern languages.
Roman architecture and engineering achievements were monumental. They perfected the arch, vault, and dome, constructing enduring structures like the Colosseum, Pantheon, and aqueducts. These engineering marvels not only showcased Roman ingenuity but also served practical purposes, from public entertainment to water supply.
A Strategic Approach: GenAI in EducationPeter Windle
Artificial Intelligence (AI) technologies such as Generative AI, Image Generators and Large Language Models have had a dramatic impact on teaching, learning and assessment over the past 18 months. The most immediate threat AI posed was to Academic Integrity with Higher Education Institutes (HEIs) focusing their efforts on combating the use of GenAI in assessment. Guidelines were developed for staff and students, policies put in place too. Innovative educators have forged paths in the use of Generative AI for teaching, learning and assessments leading to pockets of transformation springing up across HEIs, often with little or no top-down guidance, support or direction.
This Gasta posits a strategic approach to integrating AI into HEIs to prepare staff, students and the curriculum for an evolving world and workplace. We will highlight the advantages of working with these technologies beyond the realm of teaching, learning and assessment by considering prompt engineering skills, industry impact, curriculum changes, and the need for staff upskilling. In contrast, not engaging strategically with Generative AI poses risks, including falling behind peers, missed opportunities and failing to ensure our graduates remain employable. The rapid evolution of AI technologies necessitates a proactive and strategic approach if we are to remain relevant.
Unit 8 - Information and Communication Technology (Paper I).pdfThiyagu K
This slides describes the basic concepts of ICT, basics of Email, Emerging Technology and Digital Initiatives in Education. This presentations aligns with the UGC Paper I syllabus.
Operation “Blue Star” is the only event in the history of Independent India where the state went into war with its own people. Even after about 40 years it is not clear if it was culmination of states anger over people of the region, a political game of power or start of dictatorial chapter in the democratic setup.
The people of Punjab felt alienated from main stream due to denial of their just demands during a long democratic struggle since independence. As it happen all over the word, it led to militant struggle with great loss of lives of military, police and civilian personnel. Killing of Indira Gandhi and massacre of innocent Sikhs in Delhi and other India cities was also associated with this movement.
Honest Reviews of Tim Han LMA Course Program.pptxtimhan337
Personal development courses are widely available today, with each one promising life-changing outcomes. Tim Han’s Life Mastery Achievers (LMA) Course has drawn a lot of interest. In addition to offering my frank assessment of Success Insider’s LMA Course, this piece examines the course’s effects via a variety of Tim Han LMA course reviews and Success Insider comments.
Palestine last event orientationfvgnh .pptxRaedMohamed3
An EFL lesson about the current events in Palestine. It is intended to be for intermediate students who wish to increase their listening skills through a short lesson in power point.
FUNCTIONAL GROUP MODIFICATION : Medicinal Chemistry
1. TUMKUR UNIVERSITY
Department Of Studies And Research In Organic Chemistry
Seminar Presented On,
"FUNCTIONAL GROUP MODIFICATION : Medicinal
Chemistry"
Under the Guidance
Pavan Kumar. K
DOSR In Organic Chemistry
Tumkur University, Tumakuru.
Presented by
MANASA .A
Register Number : P11AZ22S104050
1st Year M.Sc., 1st Semester.
2022-2023
1
2. CONTENTS
Introduction
Functional group modification
Role of pharmocophores in functional group
Role of a functional group "Pharamacophores" in Receptor binding
of drugs
Role of functional groups in absorption and biovailiabilty
Conclusion
Reference
2
3. INTRODUCTION
Once a lead compound or a pharmacophore structure with
the desired pharmacological effect has been identified,
organic chemists can introduce modifications in the chemical
structure of the lead compound with the goal of improving
the pharmacokinetics or pharmacodynamics of a drug
candidate. These evolved structures are known as analogs.
3
5. The amino group of carbutamide was replaced by a methyl group
to give to Tolbutamide (R=CH3 : arinase) and in so doing the
antibacterial activity was seperated away from the antidiabetic
activities.
The antibacterial agent, carbutamide side effect: however it could
be not be used as an antidiabetic drug because of its antibacterial
activity which could lead to bacterial resistance.
In some cases , an experienced medical chemist knows that the
functional group will elicit a particular effect chlorothiazide (Aldo)
5
7. Consequently diazoxide (Hypeurtat) was prepared as an anti-hypertensive
drug without diuretic activity.
Obviously there is a relationship between the molecular structure of a
compound and its activity.
This phenomenon was first realized about 145 years ago.
In the above example removal of the sulfonamides side chain in chlothiazide
helped to design Diazoxide an anti-hypertensive agent without diuretic effect.
The replacement of amino group of carbutamide (antibacterial) was replaced
by methyl group to give tolbutamide(anti-diabetic agent)
7
8. Role of Pharmacophores in Functional group
For a given drug molecule functional groups play a significant role in the:
Overall water / lipid solubility.
Route of administration.
Ability to interact with specific biological targets.
Mechanism of action.
Route of metabolism and elimination.
Duration of action.
Suitability for a specific therapeutic situation.
Tendency to cause adverse effects or drug interactions.
8
9. Functional Group A : Provided ionic bond that allows this drug to interact
with its target enzyme.
Functional Group B : Interact with a zinc atom involved in normal substrate
catalysis.
Functional Group C : interact with a hydrophobic site and greatly enhance
binding.
9
Role of Functional group "Pharmacophores" in Receptor Binding of Drugs
Functional Group C
Functional Group B
Functional Group A
Enalaprilat
10. Role of Functional groups " Pharmacophores" in Absorption and
Bioavailability.
The addition of methyl group can sterically block metabolism and thus
increase the duration of action of a specific drug molecule.
This was described previously in the addition of the methyl group to . An
additional example of this concept is demonstrated when comparing
testosterone with methyltestosterone.
10
11. Testosterone is a naturally occurring androgenic hormone however, it
cannot be taken orally due to rapid oxidation of the C17 hydroxyl group to
an inactive ketone.
Addition of a methyl group at the C17 position converts the secondary
hydroxyl group into tertiary hydroxyl group. this blocks oxidative metabolism
and methyltestosterone to be administered orally.
11
12. The concept of functional groups (FGs), sets of connected atoms that can
determine the intrinsic reactivity of the parent molecule and in part are
responsible for the overall properties of the molecule, form a foundation
within modern medicinal chemistry.
Each functional group has an solubility effect, and a steric effect that needs
to be considered when evaluating the overall
pharmacodynamic and pharmacokinetic properties of any given drug
molecule.
A reaction in which functional group undergoes a change that does not
affect the number of atoms in the skeleton of the molecule.
Conclusion
13. Reference
Text book of medicinal chemistry - Volume-11. (Page number
390)
- K Ilango, P Valentina.
The organic chemistry of Drug design and drug action.
(Page number -57)
-Richard B Silvermann and Mark W Holladay.
13
