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

Bogdan Draghici; Daniela Vullo; Suleyman Akocak; Ellen A Walker; Claudiu T Supuran; Marc A Ilies

doi:10.1039/c4cc02346c

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

Chem Commun (Camb). 2014 Jun 7;50(45):5980-3. doi: 10.1039/c4cc02346c. Epub 2014 Apr 25.

Authors

Bogdan Draghici¹, Daniela Vullo, Suleyman Akocak, Ellen A Walker, Claudiu T Supuran, Marc A Ilies

Affiliation

¹ Department of Pharmaceutical Sciences and Moulder Center for Drug Discovery Research, Temple University School of Pharmacy, 3307 N Broad Street, Philadelphia, PA-19140, USA. [email protected].

PMID: 24763985
DOI: 10.1039/c4cc02346c

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

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

Substances

Enzyme Activators
Imidazoles
Isoenzymes
Carbonic Anhydrases