Synthesis of 4-methoxybenzoylhydrazones and evaluation of their antiglycation activity

Abstract

A series of 4-methoxybenzoylhydrazones 1-30 was synthesized and the structures of the synthetic derivatives elucidated by spectroscopic methods. The compounds showed a varying degree of antiglycation activity, with IC50 values ranging between 216.52 and 748.71 M, when compared to a rutin standard (IC50 = 294.46 1.50 M). Compounds 1 (IC50 = 216.52 4.2 M), 3 (IC50 = 289.58 2.64 M), 6 (IC50 = 227.75 0.53 M), 7 (IC50 = 242.53 6.1) and 11 (IC50 = 287.79 1.59) all showed more activity that the standard, and these compounds have the potential to serve as possible leads for drugs to inhibit protein glycation in diabetic patients. A preliminary SAR study was performed.