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Trypanocidal activity of conformationally restricted pentamidine congeners.

Abstract：

:A series of conformationally restricted congeners of pentamidine in which the flexible pentyl bridge of pentamidine was replaced by trans-1,2-bismethylenecyclopropyl, phenyl, pyridinyl, piperazinyl, homopiperazinyl, and piperidinyl groups were synthesized. The compounds were evaluated for trypanocidal activity in vitro and in vivo against one drug-sensitive and three drug-resistant trypanosome isolates. The DNA binding affinity of the compounds was also studied using calf thymus DNA and poly(dA-dT). The nature of the linker influenced the DNA binding affinity as well as the trypanocidal activity of the compounds. trans-1,2-Bis(4-amidinophenoxymethylene)cyclopropane (1) was over 25-fold more potent than pentamidine against the drug-resistant isolate KETRI 243As-10-3, albeit with comparable DNA binding affinity. N,N'-Bis(4-amidinophenyl)homopiperazine (8) was the most potent trypanocide in vitro against all four trypanosome isolates studied, but N,N'-bis(4-amidinophenyl)piperazine (6) was the most effective agent in vivo against both drug-sensitive and drug-resistant trypanosomes.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Donkor IO,Huang TL,Tao B,Rattendi D,Lane S,Vargas M,Goldberg B,Bacchi C

doi

10.1021/jm020375q

keywords:

subject

Has Abstract

pub_date

2003-03-13 00:00:00

pages

1041-8

issue

6

eissn

0022-2623

issn

1520-4804

journal_volume

46

pub_type

杂志文章

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