Ethylene bis-imidazoles are highly potent and selective activators for isozymes VA and VII of carbonic anhydrase, with a potential nootropic effect

被引：53
作者：
Draghici, Bogdan [1 ,2 ]
Vullo, Daniela [3 ]
Akocak, Suleyman [1 ,2 ]
Walker, Ellen A. [1 ,2 ]
Supuran, Claudiu T. [3 ]
Ilies, Marc A. [1 ,2 ]
机构：
[1] Temple Univ, Sch Pharm, Dept Pharmaceut Sci, Philadelphia, PA 19140 USA
[2] Temple Univ, Sch Pharm, Moulder Ctr Drug Discovery Res, Philadelphia, PA 19140 USA
[3] Univ Florence, Pharmaceut Sci Sect, NEUROFARBA Dept, I-50019 Florence, Italy
来源：
CHEMICAL COMMUNICATIONS | 2014年 / 50卷 / 45期
关键词：
PROTON-TRANSFER; IV ACTIVATORS; II ACTIVATION; ACTIVE-SITE; ISOFORM II; HISTIDINE; BRAIN; ENHANCEMENT; ALZHEIMERS; INHIBITOR;
D O I：
10.1039/c4cc02346c
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
A series of ethylene bis-imidazoles was synthesized via a novel microwave-mediated synthesis. Biological testing on eight isozymes of carbonic anhydrase (CA) present in the human brain revealed compounds with nanomolar potency against CA VA and CA VII, also displaying excellent selectivity against other CA isozymes present in this organ.
引用
收藏
页码：5980 / 5983
页数：4
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