Title : Synthesis and biological evaluation of 5-benzylidenerhodanine-3-acetic acid derivatives as AChE and 15-LOX inhibitors - Shafii_2015_J.Enzyme.Inhib.Med.Chem_30_389 |
Author(s) : Shafii N , Khoobi M , Amini M , Sakhteman A , Nadri H , Moradi A , Emami S , Saeedian Moghadam E , Foroumadi A , Shafiee A |
Ref : J Enzyme Inhib Med Chem , 30 :389 , 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. |
PubMedSearch : Shafii_2015_J.Enzyme.Inhib.Med.Chem_30_389 |
PubMedID: 26095345 |
Shafii N, Khoobi M, Amini M, Sakhteman A, Nadri H, Moradi A, Emami S, Saeedian Moghadam E, Foroumadi A, Shafiee A (2015)
Synthesis and biological evaluation of 5-benzylidenerhodanine-3-acetic acid derivatives as AChE and 15-LOX inhibitors
J Enzyme Inhib Med Chem
30 :389
Shafii N, Khoobi M, Amini M, Sakhteman A, Nadri H, Moradi A, Emami S, Saeedian Moghadam E, Foroumadi A, Shafiee A (2015)
J Enzyme Inhib Med Chem
30 :389