Synthesis of 4-methoxybenzoylhydrazones and evaluation of their antiglycation activity

• Published in: Molecules
• Main Author: Taha M.; Naz H.; Rasheed S.; Ismail N.H.; Rahman A.A.; Yousuf S.; Choudhary M.I.
• Format: Article
• Language: English
• Published: 2014
• Online Access: https://www.scopus.com/inward/record.uri?eid=2-s2.0-84893040474&doi=10.3390%2fmolecules19011286&partnerID=40&md5=b0cbefa20d222a483fa8cb7d79c91f7f

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.