M.Sc Chemistry - Skymount Distance Education

Use of isotopes in the bioanalysis of drugs in the drug design/drug discovery program.Qualitative andquantitative analysis of drugs: Use of IR, UV, GLC and HPLC methods. Quality controlmethods in drugmanufacture and drug formulations.DRUGS - MACROMOLECULAR TARGETSIntroduction: The concepts of macromolecular targets, Drugs acting on metabolicprocesses, cell wallsand genetic material.Drugs acting on metabolic processes: Discovery and mechanism of action ofsulfonamides, sulfonesand di aminopyrimidines. Synegism of sulfonamides and di aminopyrimidines . Synthesisofsulfapyrimidine, sulfadiazine,sulfaguanidine.Drugs acting on cell walls; Structural features of penicillins and cephalosporins. Commonbiosyntheticroute for penicillins and cephalosporin. Cell wall structure and mechanism of activity ofbeta lactamgroups of antibiotics.Natural Penicillins and their commercial preparations (outline only) Development ofsemi-synthetic andorally active penicillins, long acting penicillins. Beta lactam inhibitors. Clavulanic acidbetalactamovercomingthe development of resistance to penicillins.Cephalosporins: semi synthetic and orally active Cephalosporins. Synthesis ofcephalosporin--C andcephaline.Drug acting on genetic material: Classification into different types viz HA intercalating,DNA binding andnicking. DNA enzyme interfering, ribosomal RNA interfering and transcribing agentinhibiting drug.Drug interfering replicationDNA intercalating agents -Anticancer and anti malarials. Structure of daunomycin andadriamycin,acridines. Quinoline antimalarials. Synthesis of acridine and ellipticine.DNA binding and nicking agents - Synthesis of tinidazole and dimatridazole.DNA topoisomarase inhibitors – norfloxacin,ciprofloxain. Ofloxacin, Lome floxzacin.Synthesis ofnorfloxacin and ciprofloxacin.Inhibitors of Transcribing enzymes - Structure of rifamycin and rifampicin.Drugs interfering with Translations - Structures of Tetracyclines, Aminoglycosides,macrolide antibiotics(erythrooiycin)-Synthesis of chlcramphenicol.Antifungal agents: Structures of Griseofluvin and cyloseirine