β-lactam antibiotics work by inhibiting bacterial cell wall synthesis. There are several classes of β-lactam antibiotics including penicillins, cephalosporins, monobactams, and carbapenems. Penicillins are derived from Penicillium fungi and contain a thiazolidine ring fused to the β-lactam ring. Cephalosporins are derived from the fungus Cephalosporium and contain a dihydrothiazine ring fused to the β-lactam ring. Both penicillins and cephalosporins target bacterial transpeptidases to inhibit cell wall crosslinking. Structural modifications to these classes of β-lactams can
The all the content in this profile is completed by the teachers, students as well as other health care peoples.
thank you, all the respected peoples, for giving the information to complete this presentation.
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The all the content in this profile is completed by the teachers, students as well as other health care peoples.
thank you, all the respected peoples, for giving the information to complete this presentation.
this information is free to use by anyone.
Dear students, you can watch the Complete chapter of antibiotics in these videos as per PCI syllabus
1)Antibiotics-History & Introduction
https://www.youtube.com/watch?v=xdKch...
2)Easy Learning Of Chapter - β-Lactam antibiotics-Cephalosporin
https://www.youtube.com/watch?v=D7b5g...
3)Learn Complete Topic -β-Lactam antibiotics(Penicillin) in Medicinal Chemistry
https://www.youtube.com/watch?v=qXQ3S...
General introduction about hypertension and structure activity relationship of Different types of antihypertensive drugs, and related questions that were asked in exams.
detailed SAR and mode of action of ACE inhibitors
This ppt contains information on the classification, structures, uses and SAR related to macrolide antibiotics, lincomycins and chloramphenicol. It was prepared according to PCI syllabus for B.Pharma graduates
These are antibiotics having a macrocyclic
lactone ring with attached sugars. Erythromycin
is the first member discovered in the 1950s,
Roxithromycin, Clarithromycin and Azithromycin
are the later additions. Antimicrobial spectrum is narrow,
includes mostly gram-positive and a few gramnegative
bacteria, and overlaps considerably with
that of penicillin G. Erythromycin is highly active
against Str. pyogenes and Str. pneumoniae, N.
gonorrhoeae, Clostridia, C. diphtheriae and
Listeria, but penicillin-resistant Staphylococci
and Streptococci are now resistant to erythromycin
also.
All cocci readily develop resistance
to erythromycin, mostly by acquiring the
capacity to pump it out. Resistant Enterobacteriaceae
have been found to produce an erythromycin
esterase. Alteration in the ribosomal binding
site for erythromycin by a plasmid encoded
methylase enzyme is an important mechanism of
resistance in gram-positive bacteria. All the above
types of resistance are plasmid mediated. Change
in the 50S ribosome by chromosomal mutation
reducing macrolide binding a
penicillins - power point - History,mechanism of action,classification,chemis...Dr. Ravi Sankar
Antibiotics - Penicillin's - power point - History, mechanism of action, classification, chemistry, SAR, Nomenclature, uses, side effects- Medicinal chemistry.
Prof. P. Ravisankar M. Pharm., Ph.D.
HOD .,
Vignan Pharmacy college
vadlamudi- Guntur-A.P, India.
banuman35@gmail.com
Phone: 0 9059994000
0 9000199106
Introduction to Antibiotics,Classification,General Mechanism of action,Penicillin,Classification of Penicillin,Moa,Structure Activity Relationship,Uses
Dear students, you can watch the Complete chapter of antibiotics in these videos as per PCI syllabus
1)Antibiotics-History & Introduction
https://www.youtube.com/watch?v=xdKch...
2)Easy Learning Of Chapter - β-Lactam antibiotics-Cephalosporin
https://www.youtube.com/watch?v=D7b5g...
3)Learn Complete Topic -β-Lactam antibiotics(Penicillin) in Medicinal Chemistry
https://www.youtube.com/watch?v=qXQ3S...
General introduction about hypertension and structure activity relationship of Different types of antihypertensive drugs, and related questions that were asked in exams.
detailed SAR and mode of action of ACE inhibitors
This ppt contains information on the classification, structures, uses and SAR related to macrolide antibiotics, lincomycins and chloramphenicol. It was prepared according to PCI syllabus for B.Pharma graduates
These are antibiotics having a macrocyclic
lactone ring with attached sugars. Erythromycin
is the first member discovered in the 1950s,
Roxithromycin, Clarithromycin and Azithromycin
are the later additions. Antimicrobial spectrum is narrow,
includes mostly gram-positive and a few gramnegative
bacteria, and overlaps considerably with
that of penicillin G. Erythromycin is highly active
against Str. pyogenes and Str. pneumoniae, N.
gonorrhoeae, Clostridia, C. diphtheriae and
Listeria, but penicillin-resistant Staphylococci
and Streptococci are now resistant to erythromycin
also.
All cocci readily develop resistance
to erythromycin, mostly by acquiring the
capacity to pump it out. Resistant Enterobacteriaceae
have been found to produce an erythromycin
esterase. Alteration in the ribosomal binding
site for erythromycin by a plasmid encoded
methylase enzyme is an important mechanism of
resistance in gram-positive bacteria. All the above
types of resistance are plasmid mediated. Change
in the 50S ribosome by chromosomal mutation
reducing macrolide binding a
penicillins - power point - History,mechanism of action,classification,chemis...Dr. Ravi Sankar
Antibiotics - Penicillin's - power point - History, mechanism of action, classification, chemistry, SAR, Nomenclature, uses, side effects- Medicinal chemistry.
Prof. P. Ravisankar M. Pharm., Ph.D.
HOD .,
Vignan Pharmacy college
vadlamudi- Guntur-A.P, India.
banuman35@gmail.com
Phone: 0 9059994000
0 9000199106
Introduction to Antibiotics,Classification,General Mechanism of action,Penicillin,Classification of Penicillin,Moa,Structure Activity Relationship,Uses
The cephalosporins are β-lactam antibiotics isolated from Cephalosporium spp. or prepared semisynthetically
Most of the antibiotics introduced since 1965 have been semisynthetic cephalosporins.
Penicillin Classification, Mechanism of Action, Structure Activity Relationship, Structure of Penicillins, penicillin-binding proteins (PBPs) functional propertiesCross-linking of the peptidoglycan by transpeptidases, Cross-linking of the peptidoglycan by transpeptidases, Shape of penicillin G Penicillin SAR AcylSide Chain Modifications Instability of β-lactams to nucleophiles
Penicillinase-Resistant Penicillins Protein Binding of Penicillins
Report Back from SGO 2024: What’s the Latest in Cervical Cancer?bkling
Are you curious about what’s new in cervical cancer research or unsure what the findings mean? Join Dr. Emily Ko, a gynecologic oncologist at Penn Medicine, to learn about the latest updates from the Society of Gynecologic Oncology (SGO) 2024 Annual Meeting on Women’s Cancer. Dr. Ko will discuss what the research presented at the conference means for you and answer your questions about the new developments.
MANAGEMENT OF ATRIOVENTRICULAR CONDUCTION BLOCK.pdfJim Jacob Roy
Cardiac conduction defects can occur due to various causes.
Atrioventricular conduction blocks ( AV blocks ) are classified into 3 types.
This document describes the acute management of AV block.
Flu Vaccine Alert in Bangalore Karnatakaaddon Scans
As flu season approaches, health officials in Bangalore, Karnataka, are urging residents to get their flu vaccinations. The seasonal flu, while common, can lead to severe health complications, particularly for vulnerable populations such as young children, the elderly, and those with underlying health conditions.
Dr. Vidisha Kumari, a leading epidemiologist in Bangalore, emphasizes the importance of getting vaccinated. "The flu vaccine is our best defense against the influenza virus. It not only protects individuals but also helps prevent the spread of the virus in our communities," he says.
This year, the flu season is expected to coincide with a potential increase in other respiratory illnesses. The Karnataka Health Department has launched an awareness campaign highlighting the significance of flu vaccinations. They have set up multiple vaccination centers across Bangalore, making it convenient for residents to receive their shots.
To encourage widespread vaccination, the government is also collaborating with local schools, workplaces, and community centers to facilitate vaccination drives. Special attention is being given to ensuring that the vaccine is accessible to all, including marginalized communities who may have limited access to healthcare.
Residents are reminded that the flu vaccine is safe and effective. Common side effects are mild and may include soreness at the injection site, mild fever, or muscle aches. These side effects are generally short-lived and far less severe than the flu itself.
Healthcare providers are also stressing the importance of continuing COVID-19 precautions. Wearing masks, practicing good hand hygiene, and maintaining social distancing are still crucial, especially in crowded places.
Protect yourself and your loved ones by getting vaccinated. Together, we can help keep Bangalore healthy and safe this flu season. For more information on vaccination centers and schedules, residents can visit the Karnataka Health Department’s official website or follow their social media pages.
Stay informed, stay safe, and get your flu shot today!
Title: Sense of Smell
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the primary categories of smells and the concept of odor blindness.
Explain the structure and location of the olfactory membrane and mucosa, including the types and roles of cells involved in olfaction.
Describe the pathway and mechanisms of olfactory signal transmission from the olfactory receptors to the brain.
Illustrate the biochemical cascade triggered by odorant binding to olfactory receptors, including the role of G-proteins and second messengers in generating an action potential.
Identify different types of olfactory disorders such as anosmia, hyposmia, hyperosmia, and dysosmia, including their potential causes.
Key Topics:
Olfactory Genes:
3% of the human genome accounts for olfactory genes.
400 genes for odorant receptors.
Olfactory Membrane:
Located in the superior part of the nasal cavity.
Medially: Folds downward along the superior septum.
Laterally: Folds over the superior turbinate and upper surface of the middle turbinate.
Total surface area: 5-10 square centimeters.
Olfactory Mucosa:
Olfactory Cells: Bipolar nerve cells derived from the CNS (100 million), with 4-25 olfactory cilia per cell.
Sustentacular Cells: Produce mucus and maintain ionic and molecular environment.
Basal Cells: Replace worn-out olfactory cells with an average lifespan of 1-2 months.
Bowman’s Gland: Secretes mucus.
Stimulation of Olfactory Cells:
Odorant dissolves in mucus and attaches to receptors on olfactory cilia.
Involves a cascade effect through G-proteins and second messengers, leading to depolarization and action potential generation in the olfactory nerve.
Quality of a Good Odorant:
Small (3-20 Carbon atoms), volatile, water-soluble, and lipid-soluble.
Facilitated by odorant-binding proteins in mucus.
Membrane Potential and Action Potential:
Resting membrane potential: -55mV.
Action potential frequency in the olfactory nerve increases with odorant strength.
Adaptation Towards the Sense of Smell:
Rapid adaptation within the first second, with further slow adaptation.
Psychological adaptation greater than receptor adaptation, involving feedback inhibition from the central nervous system.
Primary Sensations of Smell:
Camphoraceous, Musky, Floral, Pepperminty, Ethereal, Pungent, Putrid.
Odor Detection Threshold:
Examples: Hydrogen sulfide (0.0005 ppm), Methyl-mercaptan (0.002 ppm).
Some toxic substances are odorless at lethal concentrations.
Characteristics of Smell:
Odor blindness for single substances due to lack of appropriate receptor protein.
Behavioral and emotional influences of smell.
Transmission of Olfactory Signals:
From olfactory cells to glomeruli in the olfactory bulb, involving lateral inhibition.
Primitive, less old, and new olfactory systems with different path
Prix Galien International 2024 Forum ProgramLevi Shapiro
June 20, 2024, Prix Galien International and Jerusalem Ethics Forum in ROME. Detailed agenda including panels:
- ADVANCES IN CARDIOLOGY: A NEW PARADIGM IS COMING
- WOMEN’S HEALTH: FERTILITY PRESERVATION
- WHAT’S NEW IN THE TREATMENT OF INFECTIOUS,
ONCOLOGICAL AND INFLAMMATORY SKIN DISEASES?
- ARTIFICIAL INTELLIGENCE AND ETHICS
- GENE THERAPY
- BEYOND BORDERS: GLOBAL INITIATIVES FOR DEMOCRATIZING LIFE SCIENCE TECHNOLOGIES AND PROMOTING ACCESS TO HEALTHCARE
- ETHICAL CHALLENGES IN LIFE SCIENCES
- Prix Galien International Awards Ceremony
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Ve...kevinkariuki227
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
The prostate is an exocrine gland of the male mammalian reproductive system
It is a walnut-sized gland that forms part of the male reproductive system and is located in front of the rectum and just below the urinary bladder
Function is to store and secrete a clear, slightly alkaline fluid that constitutes 10-30% of the volume of the seminal fluid that along with the spermatozoa, constitutes semen
A healthy human prostate measures (4cm-vertical, by 3cm-horizontal, 2cm ant-post ).
It surrounds the urethra just below the urinary bladder. It has anterior, median, posterior and two lateral lobes
It’s work is regulated by androgens which are responsible for male sex characteristics
Generalised disease of the prostate due to hormonal derangement which leads to non malignant enlargement of the gland (increase in the number of epithelial cells and stromal tissue)to cause compression of the urethra leading to symptoms (LUTS
2. Contents
• Introduction
• Classification of Antibiotics
• General structure of β-lactam antibiotics
• Structural Comparison of penicillins &
cephalosporin
• Common SAR features
• SAR of penicillins & cephalosporins
• Summary of β-lactam and subclass
3. Antibiotics
• Antibiosis (literally “against life”) as the biological concept of
survival of the fittest, in which one organism destroys another to
preserve itself.
• In 1942, Waksman defined “an antibiotic or antibiotic substance is
a substance produced by microorganisms, which has the capacity
of inhibiting the growth and even of destroying other
microorganisms.”
4. Antibiotics
Therefore, a substance is classified as an antibiotic if the
following conditions are met:
1. It is a product of metabolism
2. It is a synthetic product produced as a structural analog of a naturally
occurring antibiotic.
3. It antagonizes the growth or survival of one or more species of
microorganisms.
4. It is effective in low concentrations.
5. Chemical Classification of Antibiotics
Sr Class , Subclass & action mechanism Examples
1 β- lactam & β lactamase inhibitors
1.a Penicillins &
Cephalosporins
Cell wall cross-linking
Amoxicillin & Ampicillin
1.b Cefuroxime, Cefotaxime,
1.c β lactamase inhibitors Inactivate/ inhibit β lactamase Clavulanates, Carbapenems
2 Aminoglycosides
30 S subunit Protein synthesis &
fidelity
Kanamycin, Gentamicin,
Tobramycin,
3 Tetracycline 30 S subunit Protein synthesis
Oxytetracycline,
Demeclocycline,
4 Macrolides 50 S subunit Protein synthesis
Erythromycin, Clarithromycin,
Azithromycin
5 Lincomycins 50 S subunit Protein synthesis Lincomycin, Clindamycin
6
Peptides/
Polypeptides
Cell wall synthesis & cell membrane
functions
Vancomycin, Bacitracin,
Polymyxin B
7 Chloramphenicol Ribosomes Protein synthesis
8 Quinolones
Bacterial DNA gyrase
(Topoisomerase II)
Norfloxacin, Ciprofloxacin
9 Miscellaneous Varied Novobiocin, Linezolid
PC2ATMLinQ
10. Commercial production of antibiotics
Following a general pattern, differing in detail for each antibiotic.
The general scheme may be divided into six steps:
(a) preparation of a pure culture of the desired organism
for use in inoculation of the fermentation medium;
(b) fermentation, during which the antibiotic is formed;
(c) isolation of the antibiotic from the culture medium;
(d) purification;
(e) assays for potency, sterility, absence of pyrogens, and
other necessary data; and
(f) formulation into acceptable and stable dosage forms.
15. β-Lactam Antibiotics
• A β- lactam is a cyclic amide with four atoms in its ring.
• As the name “lactam” indicates cyclic amide which is generally considered
as analogous to the name “lactone” which is indicated for cyclic esters.
• In an older nomenclature, α was designated to the second carbon in an
aliphatic carboxylic acid/ or a carbon bears functional group such as
carboxyllic acids, and β to the third, and so on- as shown in above
structure.
• The contemporary name for this ring system is azetidinone.
• The penicillin subclass of β -lactam antibiotics is characterized by the
presence of a substituted 5-membered thiazoldine ring fused to the β -
lactam ring.
16. •The Chemical Abstracts system initiates the numbering with the sulfur atom and
assigns the ring nitrogen the 4-position.
•Thus, penicillins are named as 4-thia-l-azabicyclo[3.2.0]heptanes,
•The numbering system adopted by the USP is number 1 to the nitrogen atom and
number 4 to the sulfur atom.
•The penicillin molecule contains three chiral carbon atoms (C-3, C-5, and C-6).
•The carbon atom bearing the acylamino group (C-6) has the L configuration,
whereas the carbon to which the carboxyl group is attached has the D configuration.
Thus, the acylamino and carboxyl groups are trans to each other,
•The absolute stereochemistry of the penicillins is designated as 3S:5R:6R,
17. Units & potency
• The procedure for assay was developed at Oxford, England, and the value
became known as the
• Oxford unit: 1 Oxford unit is defined as the smallest amount of penicillin
that will inhibit, in vitro, the growth of a strain of Staphylococcus in 50 mL
of culture medium under specified conditions.
• United States Pharmacopoeia (USP) defines unit as the antibiotic activity
of 0.6 g of penicillin G sodium reference standard.
– 1 mg of penicillin G sodium is equivalent to 1,667 units,
– 1 mg of penicillin G procaine is equivalent to 1,009 units, and 1
– mg of penicillin G potassium is equivalent to 1,530 units.
20. Common SAR features
Structural requisite for antibacterial activity
• The strained β-lactam ring
• The free carboxylic acid
• The bicyclic system
– confers strain on the β-lactam ring—the greater the strain, the
greater the activity,
– but the greater the instability of the molecule to other factors.
• The acylamino side-chain
• The stereochemistry of the
– bicyclic ring with respect to the
– acylamino side-chain
21. Summarized SAR for extended spectrum of activity
Name of PC Structural change Change in activity
Ampicillin α-amino group creates an
additional chiral center
D-isomer, > L-isomer or
benzylpenicillin (2-8 times)
Hydrophilic penicillins
penetrate G-ve bacteria >
penicillin G, V, or methicillin
Amoxicillin
α-OH substitution also yields
“expanded-spectrum” with activity
and stereoselectivity similar to
that of the ampicillin group
Ampi> amoxy (2-5 times more active & acid stable)
Carbenicillin
α-Carboxybenzyl
penicillin
Incorporation of an acidic
substituent at the α-benzyl
carbon atom of penicillin G
against G-ve bacilli & resistant to
ampicillin organisms
against both β-lactamase–& non–
β-lactamase-producing G-ve
bacteria.
azlocillin, mezlocillin, and
piperacillin
α-acylureido–substituted
penicillins,
Greater activity against certain
Gram-ve bacilli than carbenicillin;
More facile penetration through
the cell envelope
Azlocillin, mezlocillin, and piperacillin> carbenicillin (certain G-ve bacilli)
22. MOA (PBP & D-alanine cross linking)
• Penicillins have a structural resemblance to two D-alanine residues linked
together, and are mistaken by the transpeptidase enzyme for D-Ala-D-Ala,
and thus incorporated into the active site.
• Once bound, the β-lactam carbonyl is attacked by the serine hydroxyl, and
ring opening occurs to leave the penicillin covalently bound to the
enzyme.
• The bulky thiazolidene ring now blocks access to the active site by either a
pentaglycine chain or water.
• As a result the penicillin becomes irreversibly bound to the transpeptidase
enzyme, preventing it from functioning properly.
• This results in incomplete cell walls that are much more fragile and
porous, and eventually lead to swelling followed by cell lysis and death.
• All β-lactam antibiotics* binds to PBPs, which are requisite for cell
wall synthesis of bacteria. PBPs are members of transpeptidases (a
subgroup of enzymes).
23.
24. Different classes of PBP’s & their role in
bacterial cell wall synthesis
Table:- Different classes of PBP’s & their role in bacterial cell wall synthesis/ formation
PBP class/ PBM Type of enzyme Role Result of inhibition
PBPs 1a &1b- first-
generation cephalosporins
Transpeptidases
in peptidoglycan synthesis
associated with cell
elongation
results in spheroplast
formation & rapid cell lysis-
PBP 2- Amdinocillin only to
PBP -2
CP’S
involved in maintaining the
rod shape of bacilli
results in ovoid /round
forms that undergo delayed
lysis
PBP 3????-
Doubtful- whether inhibition
of PBP 3 is lethal to
bacterium.
PC-G & CP’S
required for septum
formation
during cell division
in the formation of
filamentous forms
containing rod-shaped units
that cannot separate.
PBPs 4 through 6 Carboxypeptidases
responsible for the
hydrolysis of D-alanine–D-
alanine terminal peptide
bonds of the cross-linking
peptides
Apparently not lethal to the
bacterium, even though
cleavage of the terminal D-
alanine bond is required
before peptide cross-
linkage.
27. Sr
Name, Generation &
route
Structural Changes
Functional group modified
activity changed
1
Cefazolin
(1 G)^
At C-7, it possesses a tetrazoylmethylene
At C-3 thiol-containing heterocyclic
5-methyl-2-thio-1,3,4-thiadiazole.
less irritating on injection than its other
counterparts
higher serum levels,
slower renal clearance, and a longer half-life
2
Cefamandole
(2 G)^
α-hydroxyphenylacetyl (or mandoyl ) D-
mandelic acids as the acyl portion and
a thiol-containing heterocycle (5-thio-1,2,3,4-
tetrazole)
D>>>L isomer
Polar substituent in the aminoacyl moiety
β-lactamase resistant
3
Cefuroxime axetil
(2 G)*^
Alkox-imino α-methoximinoacyl–
substituted cephalosporins
esterification of the 3-carboxylic acid
acid-stable orally active ester prodrugs
lipophilic
β-lactamase–resistant
4
Cefotaxime
(3 G)^
Like cefuroxime, has a Z-methoxyimino
moiety at C-7
The oxime moiety of cefotaxime is connected
to an aminothiazole r ing
The syn-> anti-isomer is significantly more
active
Significant β-lactamase resistance
Summarized SAR for Extended spectrum of activity
28. Summary of β- lactam subclass, Target & examples
Sr AB Class, source &
Target
Sub class Examples
1 β- lactam & β lactamase inhibitors
1.a Penicillins Cell wall cross-linking
P. notatum; chrysogenum;
&
Semisynthetic
Benzyl Penicillin G
Phenoxy Penicillin V, Propicillin
Aminobenzyl Ampicillin, Amoxicillin
Penicillinase
resistant
Oxacillin, Dicloxacillin,
Flucloxacillin
Ureido PCs Mezlocillin, Piperacillin
Carboxy Ticarcillin, carbenicillin
1.b Cephalosporins Cell wall cross-linking
C. acremonium &
Semisynthetic
1 Gen Cephalexin*, Cefazolin^
2 Gen Cefuroxime*^
3 Gen Cefixime*, Cefotaxi-me^
4 Gen Cefipime^
5 Gen Ceftaroline^
1.c Beta lactamase inhibitors Inactivate/ inhibit β lactamase
Streptomyces clavuligeris.
Class I
Monobactams
Clavulanates
Class II
Carbapenems
New carbapenems