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 |
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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 |
format | Article |
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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
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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.</description><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antiparasitic agents</subject><subject>Benzamides - chemical synthesis</subject><subject>Benzamides - chemistry</subject><subject>Benzamides - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Drug Discovery</subject><subject>HAT</subject><subject>Humans</subject><subject>Inhibitor</subject><subject>Medical sciences</subject><subject>Parasitic Sensitivity Tests</subject><subject>Pharmacology. 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17 which exhibited low micromolar inhibitory potency against
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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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