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Molecules 2014, 19(1), 1286-1301; doi:10.3390/molecules19011286
Article

Synthesis of 4-Methoxybenzoylhydrazones and Evaluation of Their Antiglycation Activity

1,2,* , 1,3, 4, 1,2, 1,3, 4 and 1,4
1 Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA, Puncak Alam Campus, Shah Alam 42300, Malaysia 2 Faculty of Applied Sciences, Universiti Teknologi MARA, Shah Alam 40450, Malaysia 3 Faculty of Pharmacy, Universiti Teknologi MARA, Puncak Alam, Shah Alam 42300, Malaysia 4 Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan
* Author to whom correspondence should be addressed.
Received: 17 December 2013 / Revised: 31 December 2013 / Accepted: 2 January 2014 / Published: 21 January 2014
(This article belongs to the Section Medicinal Chemistry)
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Abstract

A series of 4-methoxybenzoylhydrazones 130 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.
Keywords: 4-methoxybenzoylhydrazones; antiglycation activity; rutin; AGEs; protein glycation inhibition; diabetes 4-methoxybenzoylhydrazones; antiglycation activity; rutin; AGEs; protein glycation inhibition; diabetes
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Taha, M.; Naz, H.; Rasheed, S.; Ismail, N.H.; Rahman, A.A.; Yousuf, S.; Choudhary, M.I. Synthesis of 4-Methoxybenzoylhydrazones and Evaluation of Their Antiglycation Activity. Molecules 2014, 19, 1286-1301.

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