Abstract
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.
Publication types
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Comparative Study
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Benzimidazoles / adverse effects
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Benzimidazoles / metabolism
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Benzimidazoles / pharmacology*
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Cations / pharmacology
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DNA / metabolism
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Disease Models, Animal
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Lung / anatomy & histology
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Lung / drug effects
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Male
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Organ Size / drug effects
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Pneumonia, Pneumocystis / drug therapy*
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Rats
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Rats, Sprague-Dawley
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Structure-Activity Relationship
Substances
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Benzimidazoles
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Cations
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DNA