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 other CA isozymes present in this organ.
Department of Pharmaceutical Sciences and Moulder Center for Drug Discovery Research, Temple University School of Pharmacy, 3307 N Broad Street, Philadelphia, PA-19140, USA. mailies@temple.edu.
Bogdan
B
Draghici
Daniela
D
Vullo
Suleyman
S
Akocak
Ellen A
EA
Walker
Claudiu T
CT
Supuran
Marc A
MA
Ilies
D001921:Brain / Q000201:enzymology; D002256:Carbonic Anhydrases / Q000378:metabolism*; D020536:Enzyme Activators / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007527:Isoenzymes / Q000378:metabolism; D007700:Kinetics; D013329:Structure-Activity Relationship
D020536:Enzyme Activators; D007093:Imidazoles; D007527:Isoenzymes; D002256:Carbonic Anhydrases