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Synthesis and Biological Evaluation of 5-Benzylidenerhodanine-3-Acetic Acid Derivatives As Ache and 15-Lox Inhibitors Publisher Pubmed



Shafii N1 ; Khoobi M2 ; Amini M2 ; Sakhteman A3 ; Nadri H3 ; Moradi A3 ; Emami S4 ; Saeedian Moghadam E2 ; Foroumadi A2 ; Shafiee A1, 2
Authors
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Authors Affiliations
  1. 1. Tehran University of Medical Sciences, International Campus (TUMS-IC), Tehran, Iran
  2. 2. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, 14176, Iran
  3. 3. Department of Medicinal Chemistry, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Iran
  4. 4. Department of Medicinal Chemistry, Faculty of Pharmacy, Mazanderan University of Medical Sciences, Sari, Iran

Source: Journal of Enzyme Inhibition and Medicinal Chemistry Published:2015


Abstract

A series of 5-benzylidenerhodanine-3-acetamides bearing morpholino-, 4-arylpiperazinyl-, or 4-benzylpiperidinyl- moieties were synthesized and their inhibitory activities against acetylcholinesterase (AChE) were evaluated. Alteration of amide part and substitution on the benzylidene moiety resulted in change of anti-AChE activity. The most active compound was the 1-benzylpiperidinyl derivative containing 4-(dimethylamino)benzylidene scaffold. Notably, the intermediate compounds, namely 5-arylidene-rhodanine-3-acetic acids (3), showed mild inhibitory activity against 15-lipoxygenase (15-LOX), while the final compound 4 showed no activity against 15-LOX. © 2015 Informa UK Ltd. All rights reserved: reproduction in whole or part not permitted.
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