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

Author : Yogita Dobhal, Ravikant Rawat, Versha Parcha, Rahul Sharma and Richa Chaudhary

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.

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