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Synthesis of 4-methoxybenzoylhydrazones and evaluation of their antiglycation activity.


ABSTRACT: 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.

SUBMITTER: Taha M 

PROVIDER: S-EPMC6271482 | biostudies-literature | 2014 Jan

REPOSITORIES: biostudies-literature

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Synthesis of 4-methoxybenzoylhydrazones and evaluation of their antiglycation activity.

Taha Muhammad M   Naz Humera H   Rasheed Saima S   Ismail Nor Hadiani NH   Rahman Aqilah Abd AA   Yousuf Sammer S   Choudhary Muhammad Iqbal MI  

Molecules (Basel, Switzerland) 20140121 1


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  ...[more]

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