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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
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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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