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

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 o...

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Bibliographic Details
Published in:Chemical communications (Cambridge, England) England), 2014-06, Vol.50 (45), p.5980-5983
Main Authors: Draghici, Bogdan, Vullo, Daniela, Akocak, Suleyman, Walker, Ellen A, Supuran, Claudiu T, Ilies, Marc A
Format: Article
Language:English
Subjects:
Brain - enzymology
Carbonic Anhydrases - metabolism
Enzyme Activators - chemical synthesis
Enzyme Activators - pharmacokinetics
Humans
Imidazoles - chemical synthesis
Imidazoles - chemistry
Imidazoles - pharmacology
Isoenzymes - metabolism
Kinetics
Structure-Activity Relationship
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Summary: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.
ISSN:1359-7345
1364-548X
DOI:10.1039/c4cc02346c