发现具有抗人类非洲锥虫病应用潜力的卤代硝基苯甲酰胺。
Discovery of halo-nitrobenzamides with potential application against human African trypanosomiasis.
机构信息
St Jude Children's Hospital, Department of Chemical Biology and Therapeutics, 262 Danny Thomas Place, Memphis, TN 38105-3678, USA.
出版信息
Bioorg Med Chem Lett. 2010 Jan 1;20(1):149-52. doi: 10.1016/j.bmcl.2009.11.022. Epub 2009 Nov 14.
PMID:19963377
Abstract
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.
摘要
一系列卤代硝基苯甲酰胺被合成并评估其抑制布氏冈比亚锥虫增殖的能力。这些化合物中有许多对寄生虫具有显著的活性，特别是 2-氯-N-(4-氯苯基)-5-硝基苯甲酰胺 17，它对 T. brucei 表现出低微摩尔抑制效力，并对疟疾和哺乳动物细胞具有选择性。
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