Metronidazole Esters: A New Class of Antiglycation Agents

Aurang      Zeb; Imran      Malik; Saima      Rasheed; Muhammad      Iqbal Choudhary; Fatima      Z. Basha

doi:10.2174/157340612802084360

Abstract

A series of metronidazole ester derivatives 1-34 has been synthesized with the aim of developing new leads with antiglycation activity. The in vitro evaluation of antiglycation potential of 1-34 showed that the ester derivatives 28, 16, and 3 have IC50 values 218.97 ± 2.5, 245.3 ± 5.1, and 278.6 ± 0.8 μM, respectively, comparable to the standard agent, rutin (IC50 = 294.5 ± 1.50 μM). The study identifies a new class of potent antiglycation agents. A structure-activity relationship has also been evaluated. All the compounds were characterized by using spectroscopic techniques, including 1H NMR, IR, and EI-MS.

Keywords: AGE, Bovin serum albumin, Protein glycation, Inhibitors, Metronidazole, Ester derivatives, spectroscopic, NMR, Schiff bases, antifungal