A Textbook of Medicinal Chemistry - III

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Publisher: Prime Publishing House
ISBN: 9789395596077
Year: 2022
Pages: 336

“Medicinal Chemistry–III” is a comprehensive and student-oriented book that presents advanced concepts of chemotherapeutic agents in a clear, simple, and well-organized manner. The book is designed to help learners understand complex topics with ease through systematic presentation, supported by diagrams, flowcharts, and structured content.

The text covers a wide range of important drug classes, including antibiotics, macrolides, antimalarials, anti-tubercular agents, quinolone antibacterials, antiviral, antifungal, antiprotozoal, and anthelmintic agents. Each section emphasizes structure–activity relationships, mechanisms of action, chemical classification, and therapeutic applications, enabling a deeper understanding of medicinal chemistry.

In addition, the book introduces key concepts of prodrug design, highlighting its applications in improving drug efficacy and safety. It also provides detailed insights into modern approaches of drug design, including quantitative structure–activity relationships (QSAR), pharmacophore modeling, and molecular considerations in drug development. The inclusion of combinatorial chemistry further enhances the understanding of contemporary techniques used in drug discovery.

Special attention has been given to exam-oriented preparation, with each chapter including question banks and multiple-choice questions to strengthen practice and confidence. With its concise yet comprehensive approach, this book serves as a valuable guide for mastering the essential and advanced aspects of medicinal chemistry while supporting academic and competitive examination preparation.

1. Antibiotics
 Antibiotics: Historical background, Nomenclature, Stereochemistry, Structure activity relationship, Chemical degradation classification and important products of the following classes.
 β-Lactam antibiotics : Penicillin, Cepholosporins, β- Lactamase inhibitors, Monobactams.
 Aminoglycosides : Streptomycin, Neomycin, Kanamycin.
 Tetracyclines: Tetracycline, Oxytetracycline, Chlortetracycline, Minocycline, Doxycycline.

2. Macrolide Antibiotics
 Antibiotics: Historical background, Nomenclature, Stereochemistry, Structure activity relationship, Chemical degradation classification and important products of the following classes.
 Macrolide: Erythromycin Clarithromycin, Azithromycin.
 Miscellaneous: Chloramphenicol*, Clindamycin.

3. Prodrug Design
 Basic concepts and application of prodrugs design.

4. Antimalarial Agents
 Antimalarial: Etiology of malaria.
 Quinolines : SAR, Quinine sulphate, Chloroquine*, Amodiaquine, Primaquine phosphate, Pamaquine*, Quinacrine hydrochloride, Mefloquine.
 Biguanides and dihydro triazines: Cycloguanil pamoate, Proguanil.
 Miscellaneous: Pyrimethamine, Artesunete, Artemether, Atovoquone

5. Anti-mycobacterial Agents (Anti tubercular agents)
 Anti-tubercular Agents :
• Synthetic anti tubercular agents : Isoniozid*, Ethionamide, Ethambutol, Pyrazinamide, Para amino salicylic acid.*
• Anti tubercular antibiotics : Rifampicin, Rifabutin, Cycloserine Streptomycine, Capreomycin sulphate.

6. Quinolone Antibacterial
 Urinary tract anti-infective agents:
 Quinolones: SAR of quinolones, Nalidixic Acid,Norfloxacin, Enoxacin, Ciprofloxacin*, Ofloxacin, Lomefloxacin, Sparfloxacin, Gatifloxacin, Moxifloxacin.

7. Antiviral Agents
 Amantadine hydrochloride, Rimantadine hydrochloride, Idoxuridine trifluoride, Acyclovir*, Gancyclovir, Zidovudine, Didanosine, Zalcitabine, Lamivudine, Loviride, Delavirding, Ribavirin, Saquinavir, Indinavir, Ritonavir.

8. Antifungal Agents
• Antifungal antibiotics : Amphotericin-B, Nystatin, Natamycin, Griseofulvin.
• Synthetic antifungal agents : Clotrimazole, Econazole, Butoconazole, Oxiconazole Tioconozole, Miconazole*, Ketoconazole, Terconazole, Itraconazole, Fluconazole, Naftifine hydrochloride, Tolnaftate*.

9. Anti-protozoal Agents
 Metronidazole*, Tinidazole, Ornidazole, Diloxanide, Iodoquinol, Pentamidine Isethionate, Atovaquone, Eflornithine
 Anthelmintics: Diethylcarbamazine citrate*, Thiabendazole, Mebendazole*, Albendazole, Niclosamide, Oxamniquine, Praziquantal, Ivermectin

10. Sulphonamides & Sulphones
 Historical development, chemistry, classification and SAR of Sulfonamides: Sulphamethizole, Sulfisoxazole, Sulphamethizine, Sulfacetamide*, Sulphapyridine, Sulfamethoxaole*, Sulphadiazine, Mefenide acetate, Sulfasalazine.
• Folate reductase inhibitors: Trimethoprim*, Cotrimoxazole.
• Sulfones: Dapsone*.

11. Drug Design
 Various approaches used in drug design.
• Physicochemical parameters used in quantitative structure activity relationship (QSAR) such as partition coefficient, Hammet’s electronic parameter, Tafts steric parameter and Hansch analysis.
• Pharmacophore modeling and docking techniques.

12. Combinatorial Chemistry
 Concept and applications chemistry: solid phase and solution phase synthesis.

A book as per the latest syllabus given by Pharmacy Council of India (PCI) New Delhi for B.Pharm students of all Indian Universities

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