N¹,N¹-Dimethyl-N³-(3-(trifluoromethyl)phenethyl)propane-1,3-diamine, a new lead for the treatment of human African trypanosomiasis

N¹,N¹-二甲基-N³-(3-(三氟甲基)苯乙基)丙烷-1,3-二胺,治疗非洲人类锥虫病的新型药物

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作者:Ngoc B Pham, Sophie Deydier, Mehdi Labaied, Séverine Monnerat, Kenneth Stuart, Ronald J Quinn

Abstract

The natural product, convolutamine I (1), has anti-trypanosomal activity however it has a high molecular weight of 473 due to a presence of 3 bromine atoms. The synthesis of the natural product convolutamine I (1) together with its analogues are presented. A SAR study against Trypanosoma brucei brucei led to compounds with improved physico-chemical properties: lower molecular weight and lower log P while maintaining potency (with a slight 2-fold improvement).

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