(2015) Synthesis and biological evaluation of 5-benzylidenerhodanine-3-acetic acid derivatives as AChE and 15-LOX inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry. pp. 389-395.
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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.
| Item Type: | Article |
|---|---|
| Keywords: | 2 5 (4 chlorobenzylidene) 4 oxo 2 thioxothiazolidin 3 yl n (1 benzylpiperidin 4 yl)acetamide; 2 5 (4 methylbenzylidene) 4 oxo 2 thioxothiazolidin 3 yl n (1 benzylpiperidin 4 yl)acetamide; 2 5 4 (dimethylamino)benzylidene] 4 oxo 2 thioxothiazolidin 3 yl] n (1 benzylpiperidin 4 yl)acetamide; 3 (2 morpholino 2 oxoethyl) 2 thioxo 5 (3,4,5 trimethoxybenzylidene)thiazolidin 4 one; 3 2 (4 benzylpiperidin 1 yl) 2 oxoethyl 5 (3 hydroxy 4 methoxybenzylidene) 2 thioxothiazolidin 4 one; 3 2 (4 benzylpiperidin 1 yl) 2 oxoethyl 5 4 (dimethylamino)benzylidene 2 thioxothiazolidin 4 one; 3 2 oxo 2 (4 phenylpiperazine 1 yl)ethyl 2 thioxo 5 (3,4,5 trimethoxybenzylidene)thiazolidin 4 one; 3 2 4 (3 fluorophenyl)piperazin 1 yl] 2 oxoethyl] 2 thioxo 5 (3,4,5 trimethoxybenzylidene)thiazolidin 4 one; 3 2 4 (3,4 dichlorophenyl)piperazin 1 yl] 2 oxoethyl] 5 (2,3 dimethoxybenzylidene) 2 thioxothiazolidin 4 one; 3 2 4 (4 fluorophenyl)piperazin 1 yl] 2 oxoethyl] 2 thioxo 5 (3,4,5 trimethoxybenzylidene)thiazolidin 4 one; 5 (4 cholorobenzylidene) 3 (2 morpholino 2oxoethyl) 2 thioxothiazolidin 4 one; 5 (4 methoxybenzylidene) 3 (2 morpholino 2 oxoethyl) 2 thioxothiazolidin 4 one; 5 benzylidenerhodanine 3 acetamide derivative; 5 benzylidenerhodanine 3 acetic acid derivative; 5 4 (dimethylamino)benzylidene 3 (2 morpholino 2 oxoethyl) 2 thioxothiazolidin 4 one; acetylcholinesterase; arachidonate 15 lipoxygenase; cholinesterase inhibitor; lipoxygenase inhibitor; rhodanine; tacrine; unclassified drug; acetic acid derivative; acetylcholinesterase; arachidonate 15 lipoxygenase; cholinesterase inhibitor; lipoxygenase inhibitor; rhodanine, aldol reaction; analytic method; Article; biological activity; clinical evaluation; drug potency; drug screening; drug structure; drug synthesis; enzyme activity; enzyme inhibition; molecular docking; priority journal; structure activity relation; structure analysis; analogs and derivatives; chemical structure; chemistry; dose response; metabolism; synthesis, Acetates; Acetylcholinesterase; Arachidonate 15-Lipoxygenase; Cholinesterase Inhibitors; Dose-Response Relationship, Drug; Lipoxygenase Inhibitors; Molecular Docking Simulation; Molecular Structure; Rhodanine; Structure-Activity Relationship |
| Page Range: | pp. 389-395 |
| Journal or Publication Title: | Journal of Enzyme Inhibition and Medicinal Chemistry |
| Volume: | 30 |
| Number: | 3 |
| Publisher: | Taylor and Francis Ltd |
| Depositing User: | ms soheila Bazm |
| URI: | http://eprints.ssu.ac.ir/id/eprint/9534 |
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