Design and Synthesis of Bioactive Compounds and their Concise Study in Therapeutic Applications

Abstract

This thesis presents new molecules and motifs designed for therapeutic applications newlinekeeping in mind the present day requirements for new sustainable drugs. The potential drug newlinecandidates which are the focal point of this study are transition metal complexes and few newlinesynthetic organic compounds. newlineAs a contribution to medicinal inorganic chemistry research, the first four working chapters newlinedeal with the therapeutic potentials of novel vanadium (IV/V), manganese (II), iron (III), newlinecobalt (III), nickel (II) and copper (II) complexes derived from ONS2and#61485; and O2N2 donor newlineligands. The complexes were newly synthesized and characterized using analytical and newlinespectroscopic techniques. These complexes were studied for their glucose uptake potential newlineand activity against drug resistant strains of bacteria and fungi (E. coli, K. pneumonia, A. newlinebaumannii, P. aeruginosa, S. aureus, C. albicans and C. neoformans). Few complexes were newlinealso studied for their anticancer potential against human breast adenocarcinoma (MCF-7), newlinehuman lung carcinoma (A549) and human cervical cancer (HeLa) cells. Additionally, the newlinecytotoxicity of these potent agents towards human embryonic kidney (HEK-293) was newlineevaluated. The activity studies were compared with the activity shown by corresponding newlineligands and standard drugs. Furthermore, the solution stability of the bioactive complexes newlineover varied pH environment were evaluated. All the compounds were evaluated for their newlinemode of interaction with a drug carrier protein, bovine serum albumin (BSA) by means of newlinespectroscopic techniques viz. fluorescence, temperature controlled UV-Visible and newlinedeconvoluted IR techniques. newlineThe last working chapter is a contribution towards medicinal organic chemistry. Herein, a newlinediscussion is presented about novel coumarin-oxime ethers and coumarin-cyclic imides as newlinetherapeutic candidates. The newly synthesized compounds have been characterised using newlineanalytical and spectroscopic tools. In vitro antitubercular activity and antidiabetic activity newlinewas established for coumarin-oxime ether and coumarin-cyclic imide conjugates newlinerespectively, the activity compared with the standard drugs. The toxicity and selectivity newlineprofile of both types of compounds are evalauted against healthy cells. Solution stability of newlinethese coumarin conjugates were also studied. They were further evaluated to elucidate their newlineinteractive behaviour with serum carrier proteins. Another part of the chapter consists newlineextensive BSA interaction studies of a known bioactive dihydropyrimidine compound to newlineevaluate its effect on drug carrier proteins. newline