Abstract

SYNTHESIS OF N-SUBSTITUTED IMIDAZOLYL AMIDO COUMARIN DERIVATIVES AS NEW DUAL M-PGES-1/5-LO INHIBITORS

Meher Unnisa*, Dr. Sruthi. K. and Prof Sumakanth. M.

ABSTRACT

mPGES-1/5-LO are the crucial enzymes that are involved in the inflammation. A new convenient synthetic method was developed for the synthesis of series of New Dual m-PGES-1/5-LO Inhibitors by hybridizing imidazolone molecule with the coumarin molecule through microwave synthesis which is considered as most green and ecofriendly synthesis and the product could be obtained within a short period of time, the advantage of microwave synthesis is; no solvent is used and if so, very minute quantity is used. Treatment of Zn dust as a catalyst leads to effective formation of amide bond with the elimination of methanol. Good yields were obtained. All the synthesized compounds were characterized by physical and spectral analysis (IR, 1H NMR, Mass spectra). NSAID’s and COX-2 Inhibitors have been used for the treatment of inflammation. However, they are associated with severe side-effects. Therefore, targeting dual enzymes m-PGES-1/5-LO and sparing gastric mucosa can be quintessential approach for the development of anti-inflammatory drugs.

Keywords: Coumarin, dual inhibition, imidazolone, mPGES-1, microwave synthesis and 5-LO.