Synthesis of 4-Methoxybenzoylhydrazones and Evaluation of Their Antiglycation Activity

摘要

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 IC_(50) values ranging between 216.52 and 748.71 μM, when compared to a rutin standard (IC_(50) = 294.46 ± 1.50 μM). Compounds 1 (IC_(50) = 216.52 ± 4.2 μM), 3 (IC_(50) = 289.58 ± 2.64 μM), 6 (IC_(50) = 227.75 ± 0.53 μM), 7 (IC_(50) = 242.53 ± 6.1) and 11 (IC_(50) = 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.