Synthesis of 4-Methoxybenzoylhydrazones and Evaluation of Their Antiglycation Activity

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 mu M, when compared to a rutin standard (IC50 = 294.46 +/- 1.50 mu M). Compounds 1 (IC50 = 216.52 +/- 4.2 mu M), 3 (IC50 = 289.58 +/- 2.64 mu M), 6 (IC50 = 227.75 +/- 0.53 mu 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.