Novel bisbenzamidines and bisbenzimidazolines as noncompetitive NMDA receptor antagonists.
A series of novel bisbenzamidines and bisbenzimidazolines with different linkers connecting the aromatic groups was tested in vitro for NMDA receptor antagonist activity. IC50 values for these compounds ranged from 1.2 to >200 microM. The bisbenzamidine with a homopiperazine ring as the central linker was found to be the most potent NMDA receptor antagonist among all the pentamidine analogues tested so far.
Tao
B
B
College of Pharmacy, Xavier University of Louisiana, New Orleans 70125, USA.
Huang
T L
TL
Sharma
T A
TA
Reynolds
I J
IJ
Donkor
I O
IO
D000818:Animals; D001550:Benzamidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D002118:Calcium / Q000378:metabolism; D002470:Cell Survival; D018698:Glutamic Acid / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D016548:Prosencephalon / Q000378:metabolism; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*
D001550:Benzamidines; D001562:Benzimidazoles; D016194:Receptors, N-Methyl-D-Aspartate; D018698:Glutamic Acid; D002118:Calcium