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Synthesis and antiprotozoal properties of pentamidine congeners bearing the benzofuran motif

Bakunov, S. A. and Bakunova, S. M. and Bridges, A. S. and Wenzler, T. and Barszcz, T. and Werbovetz, K. A. and Brun, R. and Tidwell, R. R.. (2009) Synthesis and antiprotozoal properties of pentamidine congeners bearing the benzofuran motif. Journal of Medicinal Chemistry, 52 (18). pp. 5763-5767.

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Official URL: http://edoc.unibas.ch/dok/A5843341

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Abstract

Forty-eight cationically substituted pentamidine congeners possessing benzofuran rings were synthesized by a copper mediated heteroannulation of substituted o-iodophenols with phenyl acetylenes. Activities of compounds 1-48 against Trypanosoma brucei rhodesiense, Plasmodium falciparum, and Leishmania donovani and cytotoxicities for mammalian cells were influenced by the nature of cationic substituents, placement of the benzofuran fragment, and the length of the carbon linker between aromatic moieties. Several dications exhibited superior antiplasmodial and antileishmanial potencies compared to pentamidine
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Brun, Reto and Wenzler, Tanja
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:American Chemical Society
ISSN:0022-2623
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:13 Sep 2018 14:21
Deposited On:14 Sep 2012 06:41

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