Journal of Bioequivalence & Bioavailability

Stereoselective synthesis, characterization & biological evaluation of novel geometrical isomers of imidazolones

3^rd World Congress Bioavailability & Bioequivalence

March 26-28, 2012 Marriott Hotel & Convention Centre, Hyderabad, India

Anitha.S1, Gopinath.N, Sundari CH B T and NJP Subhashini

Posters: J Bioequiv Availab

Abstract:

S ynthesis and separation of geometrical isomers (E/Z) can provide greater selectivity for their biological targets, improved therapeutic indices an d better pharmacokinetics than a mixture of diastereomers.Imidazolinones were reported to possess anti-microbial, analgesic, anti hyperlipidemic, anti-viral, anti-HIV, sedative-hypnotic, anti-convulsant, anti-inflammatory, anti- tumour, anti-oxidant, and anti-helmenthicactivites. In this view phenylacrylamidesandimidazolonederivatives were synthesized from oxazolones. Structures of these compounds were confirmed by IR, NMR, MS and LC-MS. Imidazoloneswere obtained as a mixture of geometrical isomers, among them major isomers were separated. Both phenylacrylamide derivatives and imidazolones were evaluated for DNA binding, antioxidant and other biological studies and found to have good biological activities. As the single enantiomers and stereoisomers have overtaken racemic molecules in the percentage of approved drugs in the market, the separation and quantification of stereoisomers is therefore of great importance,especially in pharmaceutical industries