Antibiotics & Antimalarials: Structures & SAR Notes [U-2]

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Antibiotics Notes

Macrolides

Various Macrolides Drugs

Various Miscellaneous Antibiotics

Prodrugs

Basic Concept of Prodrugs

Antimalarials

Various Quinolines drugs

Various Biguanides and Dihydrotriazines Drugs

Cycloguanil Pamoate
Proguanil

Various Miscellaneous Antimalarials Drugs

Other Units of Medicinal Chemistry III

Medicinal Chemistry III

Other Subjects of B Pharmacy 6th Semester

Topic wise notes of:

Herbal Drug Technology

Herbal Raw Materials & Indian Medicine Systems
Nutraceuticals: Uses, Herbs & Interactions
Herbal Cosmetics, Excipients & Formulations
Herbal Drug Evaluation, Patents & Regulations
Herbal Industry: Scope, GMP & Infrastructure

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Topic wise notes of:

Biopharmaceutics and Pharmacokinetics

Biopharmaceutics: Absorption & Distribution
Drug Elimination, Bioavailability & Bioequivalence
Pharmacokinetics Models, Dosing & Parameters
Multicompartment models
Nonlinear Pharmacokinetics

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Pharmacology III

Respiratory & GI Tract Drug Pharmacology
Chemotherapy: Principles & Key Antibiotics
Chemotherapy: TB, Fungal & Parasitic Drugs
UTIs, Cancer Chemo & Immunopharmacology
Toxicology Basics & Chrono pharmacology

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Topic wise notes of:

Pharmaceutical Biotechnology

Introduction to Pharmaceutical Biotechnology
Genetic Engineering & rDNA Technology
Immunology and Vaccine Technology
Microbial Genetics & Biotransformation
Fermentation & Bioproduct Production

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Topic wise notes of:

Pharmaceutical Quality Assurance

Quality Assurance, GMP, ICH, QbD & Quality System
GMP: Personnel, Premises & Equipment Control
Quality Control and Good Laboratory Practice
Complaints & Document Management
Calibration and Warehousing

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Summary of Antibiotics and Antimalarials Notes

1. Antibiotics

Historical Background: Discovery and evolution of antibiotics; major milestones.
Nomenclature: Based on source, structure, or microbial target.
Stereochemistry: Crucial for biological activity and selectivity.
Structure-Activity Relationship (SAR): Understanding chemical groups essential for activity.
Chemical Degradation: Hydrolysis, oxidation, and photodegradation pathways.
Classification & Key Products:
- Chlortetracycline: Tetracycline class; broad-spectrum activity.
- Macrolides:
  - Erythromycin: 14-membered ring; bacteriostatic.
  - Clarithromycin, Azithromycin: Semi-synthetic derivatives with improved stability.
- Miscellaneous:
  - Chloramphenicol: Broad-spectrum; risk of aplastic anemia.
  - Clindamycin: Lincosamide; effective against anaerobes.

2. Prodrugs

Concept: Inactive compounds metabolized into active forms.
Application: Improve solubility, absorption, and targeted delivery.

3. Antimalarials

Etiology: Malaria caused by Plasmodium species.

4. Quinolines

SAR and examples:
- Quinine, Chloroquine, Amodiaquine, Primaquine, Pamaquine, Quinacrine, Mefloquine.

5. Biguanides & Triazines

Cycloguanil, Proguanil: Inhibit parasite folate pathway.

6. Miscellaneous

Pyrimethamine, Artesunate, Artemether, Atovaquone: Target various parasite life stages

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