Synthesis of 4-Methoxybenzoylhydrazones and Evaluation of Their Antiglycation Activity

Molecules

Muhammad Taha²  Humera Naz²  Saima Rasheed¹  Nor Hadiani Ismail²  Aqilah Abd Rahman²  Sammer Yousuf¹ 

[1] H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan;Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA, Puncak Alam Campus, Shah Alam 42300, Malaysia

关键词: 4-methoxybenzoylhydrazones;    antiglycation activity;    rutin;    AGEs;    protein glycation inhibition;    diabetes;   

DOI  :  10.3390/molecules19011286

来源: mdpi

【 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 IC₅₀ values ranging between 216.52 and 748.71 µM, when compared to a rutin standard (IC₅₀ = 294.46 ± 1.50 µM). Compounds 1 (IC₅₀ = 216.52 ± 4.2 µM), 3 (IC₅₀ = 289.58 ± 2.64 µM), 6 (IC₅₀ = 227.75 ± 0.53 µM), 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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.