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
收藏
页码：389 / 395
页数：7
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