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Synthesis and antiprotozoal properties of pentamidine congeners bearing the benzofuran motif.

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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Bakunov SA,Bakunova SM,Bridges AS,Wenzler T,Barszcz T,Werbovetz KA,Brun R,Tidwell RR

doi

10.1021/jm9006406

subject

Has Abstract

pub_date

2009-09-24 00:00:00

pages

5763-7

issue

18

eissn

0022-2623

issn

1520-4804

journal_volume

52

pub_type

杂志文章

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