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Discovery of nitroheterocycles active against African trypanosomes. In vitro screening and preliminary SAR studies.

Abstract：

:A selection of 76 nitroheterocycles and related compounds from our in-house compound library was screened in vitro against the parasite Trypanosoma brucei rhodesiense, causative agent of human African trypanosomiasis (HAT). The unspecific cytotoxicity of the compounds was also evaluated against rat myoblast L6-cells to measure the selectivity of the compounds towards the parasite. This screening revealed some preliminary structure-activity relationships (SAR) among the series, and six hit compounds showing interesting activity (IC(50)≤10μM) and fair selectivity (SI>17). The 7-nitroquinoxalin-2-one and 5-nitroindazole scaffold derivatives 58 and 35, respectively, are particularly interesting because of their established oral bioavailability in mice. These hits represent interesting starting points for a medicinal project aimed at identifying the SAR behind this class of compounds.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Arán VJ,Kaiser M,Dardonville C

doi

10.1016/j.bmcl.2012.06.004

subject

Has Abstract

pub_date

2012-07-15 00:00:00

pages

4506-16

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00742-1

journal_volume

22

pub_type

杂志文章

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