Synthesis and biological evaluation of 5-benzylidenerhodanine-3-acetic acid derivatives as AChE and 15-LOX inhibitors

被引：22

作者：

Shafii, Negah ^{[1
]}

Khoobi, Mehdi ^{[2
,3
]}

Amini, Mohsen ^{[2
,3
]}

Sakhteman, Amirhossein ^{[4
]}

Nadri, Hamid ^{[4
]}

Moradi, Alireza ^{[4
]}

Emami, Saeed ^{[5
,6
]}

Moghadam, Ebrahim Saeedian ^{[2
,3
]}

Foroumadi, Alireza ^{[2
,3
]}

Shafiee, Abbas ^{[1
,2
,3
]}

机构：

[1] Univ Tehran Med Sci, Tehran 14176, Iran

[2] Univ Tehran Med Sci, Fac Pharm, Dept Med Chem, Tehran 14176, Iran

[3] Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Tehran 14176, Iran

[4] Shahid Sadoughi Univ Med Sci, Dept Med Chem, Fac Pharm, Yazd, Iran

[5] Mazanderan Univ Med Sci, Dept Med Chem, Sari, Iran

[6] Mazanderan Univ Med Sci, Pharmaceut Sci Res Ctr, Fac Pharm, Sari, Iran

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2015年 / 30卷 / 03期

关键词：

2-Thioxothiazolidin-4-one; 15-lipoxygenase; acetylcholinesterase; docking study; inhibitors; rhodanines; ALDOSE REDUCTASE INHIBITOR; TAU AGGREGATION INHIBITORS; ANTIFUNGAL ACTIVITY; ACETYLCHOLINESTERASE; RHODANINE; DOCKING; SERIES;

D O I：

10.3109/14756366.2014.940935

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：389 / 395

页数：7

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