Unit 1
Physicochemical properties of drugs in relation to biological actionAcid-Base Properties, Water solubility, Partition coefficient, drug administration, drug distribution, metabolism (Phase I and Phase II) and toxicity of drug receptor interaction, conformational flexibility and multiple mode of action, optical isomerism and biological activity, selected physico-chemical properties (Ionization, hydrogen bonding and biological action, chelation and biological action, oxidation – reduction potential and biological action, absorption and orientation at surfaces) Enzymes, hormones and Vitamins – representative cases, nomenclature, classification and characteristics of enzymes, mechanism of enzyme action, factors affecting enzyme action, cofactors and co-enzymes, enzymes in organic synthesis, mechanism of enzyme catalysis, enzyme inhibition.
Unit 2
Essentials of drug designMolecular mimetics, drug-lead modification, drug design using QSAR and computer assisted design, assessment of drug activity, receptors and drug action, mechanism of drug action, drug metabolism pathways, Drug potentiation, drug antagonism and drug resistance
Unit 3
Silicon in medicinal chemistryOrganosilicon molecules with medicinal applications, chemical properties of organic silicon relevant for medicinal chemistry, silicon containing amino acids and analogues, Organosilicon based fluoride acceptors for imaging, Trialkyl silyl derivatives of drugs and biologically active molecules, Hydrophobic quaternary silanes, Increased hydrophobicity of silyl groups & effect on biological activity,
Unit 4
Silicon derivativesDisilyl&disilacyclic compounds & related derivatives, spirosilanes& other silacyclic derivatives, Diphenyl silane derivatives, Silyl groups as isosteres of quaternary ammonium groups, Silyl ethers as hydrophobic substituents, silicates, silanols, silanediols&silanetriols, Hypervalent silicon compounds, stability of organo silicon compounds, silyl ethers and drug delivery strategies related to silicon, metabolism of organosilicon molecules.
Unit 5
Medicinal agentsMedicinal agents belonging to alkaloids, steroids, polypeptides, modified nucleic acid bases, sulphonamide and sulpha drugs, antibacterials – sulpha drugs, substituted sulphonamides, anticonvulsants, anticoagulants, antiamoebic agents, antihelmintic agents, anti-malarial agents, diuretics and cardio vascular agents, drugs for AIDS, medicinal agents affecting CNS, analgesics, antipyretics, antiseptics and disinfectants.