Discovery of halo-nitrobenzamides with potential application against human African trypanosomiasis

A series of halo-nitrobenzamide were synthesized and evaluated for their ability to block proliferation of Trypanosoma brucei brucei. A number of these compounds had significant activity against the parasite, particularly 2-chloro- N-(4-chlorophenyl)-5-nitrobenzamide 17 which exhibited low micromola...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010, Vol.20 (1), p.149-152
Hauptverfasser: Hwang, Jong Yeon, Smithson, David, Connelly, Michele, Maier, Julie, Zhu, Fangyi, Guy, Kiplin R.
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container_end_page 152
container_issue 1
container_start_page 149
container_title Bioorganic & medicinal chemistry letters
container_volume 20
creator Hwang, Jong Yeon
Smithson, David
Connelly, Michele
Maier, Julie
Zhu, Fangyi
Guy, Kiplin R.
description A series of halo-nitrobenzamide were synthesized and evaluated for their ability to block proliferation of Trypanosoma brucei brucei. A number of these compounds had significant activity against the parasite, particularly 2-chloro- N-(4-chlorophenyl)-5-nitrobenzamide 17 which exhibited low micromolar inhibitory potency against T. brucei and selectivity towards both malaria and mammalian cells.
doi_str_mv 10.1016/j.bmcl.2009.11.022
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source MEDLINE; Access via ScienceDirect (Elsevier)
subjects Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiparasitic agents
Benzamides - chemical synthesis
Benzamides - chemistry
Benzamides - pharmacology
Biological and medical sciences
Drug Discovery
HAT
Humans
Inhibitor
Medical sciences
Parasitic Sensitivity Tests
Pharmacology. Drug treatments
Trypanocidal Agents - chemical synthesis
Trypanocidal Agents - chemistry
Trypanocidal Agents - pharmacology
Trypanosoma brucei brucei
Trypanosoma brucei brucei - drug effects
Trypanosomiasis
Trypanosomiasis, African - drug therapy
title Discovery of halo-nitrobenzamides with potential application against human African trypanosomiasis
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