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 micromolar inhibitory potency against T. brucei and selectivity towards both malaria and mammalian cells.
Hwang
Jong Yeon
JY
St Jude Children's Hospital, Department of Chemical Biology and Therapeutics, 262 Danny Thomas Place, Memphis, TN 38105-3678, USA.
Smithson
David
D
Connelly
Michele
M
Maier
Julie
J
Zhu
Fangyi
F
Guy
Kiplin R
KR
D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D055808:Drug Discovery; D006801:Humans; D021261:Parasitic Sensitivity Tests; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D014346:Trypanosoma brucei brucei / Q000187:drug effects; D014353:Trypanosomiasis, African / Q000188:drug therapy
C549132:2-chloro-N-(4-chlorophenyl)-5-nitrobenzamide; D001549:Benzamides; D014344:Trypanocidal Agents