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.
Format:	Artikel
Sprache:	eng
Schlagworte:	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
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2009.11.022