Activity of cationically substituted bis-benzimidazoles against experimental Pneumocystis carinii pneumonia.
On the basis of a previously observed correlation between the antimicrobial activity and DNA binding strength of dicationic molecules, a series of 10 dicationically substituted bis-benzimidazoles were tested for activity in the rat model of Pneumocystis carinii pneumonia. One of the compounds, 1,4-bis[5-(2-imidazolinyl)-2-benzimidazolyl]butane, was found to be more potent and less toxic than pentamidine.
Tidwell
R R
RR
Department of Pathology, School of Medicine, University of North Carolina, Chapel Hill 27599.
Jones
S K
SK
Naiman
N A
NA
Berger
L C
LC
Brake
W B
WB
Dykstra
C C
CC
Hall
J E
JE
D000818:Animals; D001562:Benzimidazoles / Q000009:adverse effects / Q000378:metabolism / Q000494:pharmacology*; D002412:Cations / Q000494:pharmacology; D004247:DNA / Q000378:metabolism; D004195:Disease Models, Animal; D008168:Lung / Q000033:anatomy & histology / Q000187:drug effects; D008297:Male; D009929:Organ Size / Q000187:drug effects; D011020:Pneumonia, Pneumocystis / Q000188:drug therapy*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
D001562:Benzimidazoles; D002412:Cations; D004247:DNA