Activity of cationically substituted bis-benzimidazoles against experimental Pneumocystis carinii pneumonia

Author:

Tidwell R R1,Jones S K1,Naiman N A1,Berger L C1,Brake W B1,Dykstra C C1,Hall J E1

Affiliation:

1. Department of Pathology, School of Medicine, University of North Carolina, Chapel Hill 27599.

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.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Reference24 articles.

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3. Bell C. A. C. C. Dykstra N. A. Naiman M. Cory T. A. Fairley and R. R. Tidwell. Structure-activity studies of dicationic substituted bisbenzimidazoles against Giardia lamblia: correlation of antigiardiAl activity with DNA binding affinity and giardial topoisomerase II inhibition. Submitted for publication.

4. Structure-activity relationships of analogs of pentamidine against Plasmodium falciparum and Leishmania mexicana amazonensis;Bell C. A.;Antimicrob. Agents Chemother.,1990

5. Inhibition of Cryptosporidium parvum in neonatal Hsd:(ICR)BR Swiss mice by polyether ionophores and aromatic amidines;Blagburn B. L.;Antimicrob. Agents Chemother.,1991

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