This course from pharmaceutical chemistry domain provides a comprehensive overview of the key concepts of medicinal chemistry. Course will comprise of basic principles of drug designing and eventually with more emphasis on structural activity relationship (SAR) of molecules that are pharmaceutically important. Course will also cover basic principles of in silico drug designing. It aims to explain the synthesis of different classes of drugs and their pharmacophores.
COURSE LEARNING OUTCOMES (CLO)
CLO: 1. To describe the fundamentals of medicinal chemistry, structural activity relationship (SAR) of different pharmacophores
CLO: 2. To illustrate principles and steps for synthesis of different classes of drugs, and their use
CLO: 3. To apply knowledge of basic concepts of medicinal chemistry for designing of different pharmacophores
- INTRODUCTION TO MEDICINAL CHEMISTRY:
- Chemical constitution and biological activity: (Receptor, Theory, Structure Activity Relationships (SAR) and Drug Metabolism). Modern concept of rational drug design, pro drug, combinatorial chemistry and computer aided drug design (CADD) and concept of antisense molecules.
- DRUG TARGETS AND DRUG DESIGNING:
- Introduction and types of drug targets
- Introduction to molecular modeling and computational chemistry
- Structure based designing
- Ligand-based designing
- Various techniques in drug synthesis
- GENERAL PROPERTIES, CHEMISTRY, BIOLOGICAL ACTION, STRUCTURE ACTIVITY RELATIONSHIP AND THERAPEUTIC APPLICATIONS OF THE FOLLOWING
- _Steroidal Hormones (Testosterone, Progesterone, Estrogen, Aldosterone and Cortisol), Proteinous Hormones (Insulin, Glucagon, Oxytocin and Vasopressin)_
- Anti-neoplastic Agents: Tamoxifen, Fluorouracil, Mercaptopurine, Methotrexate and Vincristine.
Sedatives and Hypnotics: Benzodiazepines, Barbiturates, Paraldehyde, Glutethimide, Chloral hydrate, and alcohols.
- Sedatives & Hypnotics: Benzodiazepines, Barbiturates, Paraldehyde, Glutethimide, Chloral hydrate, and alcohols.
- _Local anaesthetics (Procaine, Lignocaine, Eucaine, Cocaine and Benzocaine), General anaesthetics (Cyclopropane, Halothane, Nitrous oxide, Chloroform, Thiopental Sodium, Ketamine, Methohexital, Thioamylal Sodium, Fantanyl Citrate, Tribromo ethanol)_
- Analgesics and Antipyretics: Paracetamol, Salicylic acid analogues, Quinolines derivatives, Pyrazolone and Pyrazolodiones, N – arylanthranilic acids, Aryl and heteroaryl acetic acid derivatives.