MEDICINAL CHEMISTRY – III (Theory)

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Course Name : MEDICINAL CHEMISTRY – III (Theory)

Code(Credit) : BPHT3201(4-0-0)

Course Objectives

  • This subject is designed to impart fundamental knowledge on the structure, chemistry and therapeutic value of drugs. The subject emphasis on modern techniques of
    rational drug design like quantitative structure activity relationship (QSAR), Prodrug
    concept, combinatorial chemistry and Computer aided drug design (CADD). The subject
    also emphasizes on the chemistry, mechanism of action, metabolism, adverse effects,
    Structure Activity Relationships (SAR), therapeutic uses and synthesis of important
    drugs.

Learning Outcomes

  • Upon completion of the course student shall be able to
    1. Understand the importance of drug design and different techniques of drug
    design.
    2. Understand the chemistry of drugs with respect to their biological activity. 3. Know the metabolism, adverse effects and therapeutic value of drugs.
    4. Know the importance of SAR of drugs.

Course Syllabus

UNIT – I
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
UNIT – II
Antibiotics
Historical background, Nomenclature, Stereochemistry, Structure activity
relationship, Chemical degradation classification and important products of
the following classes.
126
Macrolide: Erythromycin Clarithromycin, Azithromycin.
Miscellaneous: Chloramphenicol*, Clindamycin.
Prodrugs: Basic concepts and application of prodrugs design.
Antimalarials: 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.
UNIT – III
Anti-tubercular Agents
Synthetic anti tubercular agents: Isoniozid*, Ethionamide, Ethambutol,
Pyrazinamide, Para amino salicylic acid.*
Anti tubercular antibiotics: Rifampicin, Rifabutin, Cycloserine
Streptomycine, Capreomycin sulphate.
Urinary tract anti-infective agents
Quinolones: SAR of quinolones, Nalidixic Acid,Norfloxacin, Enoxacin,
Ciprofloxacin*, Ofloxacin, Lomefloxacin, Sparfloxacin, Gatifloxacin,
Moxifloxacin
Miscellaneous: Furazolidine, Nitrofurantoin*, Methanamine. Antiviral agents:
Amantadine hydrochloride, Rimantadine hydrochloride, Idoxuridine
trifluoride, Acyclovir*, Gancyclovir, Zidovudine, Didanosine, Zalcitabine,
Lamivudine, Loviride, Delavirding, Ribavirin, Saquinavir, Indinavir,
Ritonavir.
UNIT – IV 08 Hours
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*. Anti-protozoal Agents: Metronidazole*, Tinidazole, Ornidazole, Diloxanide, Iodoquinol, Pentamidine Isethionate, Atovaquone, Eflornithine.
Anthelmintics: Diethylcarbamazine citrate*, Thiabendazole, Mebendazole*,
Albendazole, Niclosamide, Oxamniquine, Praziquantal, Ivermectin.
127
Sulphonamides and Sulfones
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*.
UNIT – V
Introduction to 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. Combinatorial Chemistry: Concept and applications
chemistry: solid phase and solution phase synthesis.
of combinatorial

Session Plan

Session 1

Antibiotics
Historical background, Nomenclature, Stereochemistry, Structure activity
relationship, Chemical degradation classification and important products of
the followingpenicillin,cephallosporine, beta-lactamase, monobactam

Session 2

β-Lactam antibiotics: Penicillin, Cepholosporins, β- Lactamase inhibitors,
Monobactams
Aminoglycosides: Streptomycin, Neomycin, Kanamycin

penicillin,cephallosporine, beta-lactamase, monobactam

Session 11

Anti tubercular antibiotics: Rifampicin, Rifabutin, Cycloserine
Streptomycine, Capreomycin sulphate.
Urinary tract anti-infective agents
Quinolones: SAR of quinolones, Nalidixic Acid,Norfloxacin, Enoxacin,
Ciprofloxacin*, Ofloxacin, Lomefloxacin, Sparfloxacin, Gatifloxacin,
Moxifloxacin

https://www.youtube.com/watch?v=sk1uf6CaE8M

https://www.youtube.com/watch?v=8PXr9RCFiLs

https://www.youtube.com/watch?v=suoPHa2z4L4

Session 10

Anti-tubercular Agents
Synthetic anti tubercular agents: Isoniozid*, Ethionamide, Ethambutol,
Pyrazinamide, Para amino salicylic acid.*

https://www.youtube.com/watch?v=wUJJ5F12C5s

Session 8

Miscellaneous: Pyrimethamine, Artesunete, Artemether, Atovoquone.

https://pharmawiki.in/b-pharmacy-3rd-year-subjects-syllabus-pdf-b-pharm-second-year-5-6-semester/

Session 7

Quinolines: SAR, Quinine sulphate, Chloroquine*, Amodiaquine, Primaquine phosphate, Pamaquine*, Quinacrine hydrochloride, Mefloquine. Biguanides and dihydro triazines: Cycloguanil pamoate, Proguanil.

https://gpatindia.com/chloroquine-synthesis-sar-mcqstructurechemical-properties-and-therapeutic-uses/

Session 6

Prodrugs: Basic concepts and application of prodrugs design.
Antimalarials: Etiology of malaria.

https://www.youtube.com/watch?v=jeJr_56-VH0

https://mcwhealthcare.com/malaria/

Session 5

Macrolide: Erythromycin Clarithromycin, Azithromycin.
Miscellaneous: Chloramphenicol*, Clindamycin.

Macrolide

https://www.youtube.com/watch?v=PvSNGf8jGEs

Session 4

Antibiotics
Historical background, Nomenclature, Stereochemistry, Structure activity
relationship, Chemical degradation classification and important products of
the following

cephalosporine, beta-lactamase, Monobactam

https://www.khanacademy.org/science/organic-chemistry/carboxylic-acids-derivatives/acid-derivatives-jay/v/beta-lactam-antibiotics

Session 3

Tetracyclines: Tetracycline,Oxytetracycline, Chlortetracycline, Minocycline, Doxycycline

Tetracycline-converted

Session 12

Miscellaneous: Furazolidine, Nitrofurantoin*, Methanamine. Antiviral agents:
Amantadine hydrochloride, Rimantadine hydrochloride, Idoxuridine
trifluoride, Acyclovir*, Gancyclovir, Zidovudine, Didanosine, Zalcitabine,
Lamivudine, Loviride, Delavirding, Ribavirin, Saquinavir, Indinavir,
Ritonavir.

https://www.youtube.com/watch?v=1inyGyecT8I

https://pharmawiki.in/b-pharmacy-3rd-year-subjects-syllabus-pdf-b-pharm-second-year-5-6-semester/

Session 13

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*.https://pharmawiki.in/b-pharmacy-3rd-year-subjects-syllabus-pdf-b-pharm-second-year-5-6-semester/

https://www.osmosis.org/learn/Miscellaneous_antifungal_medications

Session 14

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

https://www.youtube.com/watch?v=UmXMxh9jf80

https://pharmawiki.in/b-pharmacy-3rd-year-subjects-syllabus-pdf-b-pharm-second-year-5-6-semester/

https://www.youtube.com/watch?v=55E8whgoa9o

Session 15

Sulphonamides and Sulfones
Historical development, chemistry, classification and SAR of Sulfonamides:
Sulphamethizole, Sulfisoxazole, Sulphamethizine, Sulfacetamide*,
Sulphapyridine, Sulfamethoxaole*, Sulphadiazine, Mefenide acetate, Sulfasalazine.

https://www.youtube.com/watch?v=jZpygjtqm28

Session 16

Folate reductase inhibitors: Trimethoprim*, Cotrimoxazole.
Sulfones: Dapsone*.

https://www.youtube.com/watch?v=_cu45SQfl24

https://www.youtube.com/watch?v=iVZZMJDfI7k

Session 17

Introduction to 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

https://slideplayer.com/slide/5943789/

Session 18

Pharmacophore modeling and docking techniques. Combinatorial Chemistry: Concept and applications
chemistry: solid phase and solution phase synthesis.

https://www.youtube.com/watch?v=hU7UmrHo0O4

References

Recommended Books (Latest Editions)
1. Wilson and Giswold’s Organic medicinal and Pharmaceutical Chemistry.

2. Foye’s Principles of Medicinal Chemistry.

3. Burger’s Medicinal Chemistry, Vol I to IV.
4. Introduction to principles of drug design- Smith and Williams.
5. Remington’s Pharmaceutical Sciences.

Foye's Principles of Medicinal Chemistry eBook by Victoria Roche - 9781496385871 | Rakuten Kobo United States

Our Main Teachers

A Avinash

Asst Professor
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A.Avinash working as Assistant Professor, Dept of CSE, Centurion University of Technology and Management, Andhra Pradesh . Interested to work on Machine learning,Natural Language Processing,Problem Solving Methodologies , and ChatBot. Programming Skill: C Programming Data Structure Object Oriented Programming using C++ Formal Language Automata Theory Python Web Development(HTML,CSS,PHP) Database Management Systems Compilers