Design, synthesis and evaluation of phenyl oxazolone derivatives as cardioprotective drugs

Abstract

In the present study oxazolone derivatives were prepared with substitution of amine propanol side chain at position 4 of 2-phenyl-5-oxazolones. The synthesized compounds were characterized on basis of spectral studies and explored for cardioprotective effect. Substituted oxazolone derivatives have been prepared by condensation of hipuric acid with p-amino benzaldehyde in presence of ethanol, acetic anhydride and sodium acetate.the prepared intermediate fused with epichlorhydrin moiety to synthesize 4-[2-(oxiran-2-yl methylamino)benzylidene]-2-phenyloxazol-5-(4H)-one. Then five different amino derivatives (VIA-VIE) were synthesized. Furthermore, the synthesized compounds were evaluated for cardioprotective activity. The structures of the synthesized compounds were assigned on the basis of UV, IR, and ¹H NMR data. The synthesized compounds were at dose level of 50 mg/kg body weight screened for cardioprotective activity and compared to standard ramipril at dose level of 1 mg/kg body weight. From the above studies it could be concluded that condensed product oxazolone and amino propanol showed significant (P<0.05) cardioprotective effect.