Synthesis and Antiprotozoal Properties of Pentamidine Congeners Bearing the Benzofuran Motif

被引：26

作者：

Bakunov, Stanislav A. ^{[1
]}

Bakunova, Svetlana M. ^{[1
]}

Bridges, Arlene S. ^{[1
]}

Wenzler, Tanja ^{[3
]}

Barszcz, Todd ^{[2
]}

Werbovetz, Karl A. ^{[2
]}

Brun, Reto ^{[3
]}

Tidwell, Richard R. ^{[1
]}

机构：

[1] Univ N Carolina, Sch Med, Dept Pathol & Lab Med, Chapel Hill, NC 27599 USA

[2] Ohio State Univ, Coll Pharm, Div Med Chem & Pharmacognosy, Columbus, OH 43210 USA

[3] Swiss Trop Inst, Dept Med Parasitol & Infect Biol, CH-4002 Basel, Switzerland

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 18期

关键词：

HUMAN AFRICAN TRYPANOSOMIASIS; CHEMOTHERAPY; FUTURE;

D O I：

10.1021/jm9006406

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：5763 / 5767

页数：5

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