N¹,N¹-Dimethyl-N³-(3-(trifluoromethyl)phenethyl)propane-1,3-diamine, a new lead for the treatment of human African trypanosomiasis.
N¹,N¹-Dimethyl-N³-(3-(trifluoromethyl)phenethyl)propane-1,3-diamine, a new lead for the treatment of human African trypanosomiasis.
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N·,N·1-二甲基-N·3-(3-(三氟甲基)苯乙基)丙烷-1,3-二胺,一种治疗非洲人类锥虫病的新先导药物。
DOI:
10.1016/j.ejmech.2013.12.050
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发表时间:
2014
影响因子:
6.7
通讯作者:
Quinn,RonaldJ
中科院分区:
文献类型:
--
作者:
Pham,NgocB;Deydier,Sophie;Labaied,Mehdi;Monnerat,Séverine;Stuart,Kenneth;Quinn,RonaldJ
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 againstTrypanosoma brucei bruceiled to compounds with improved physico-chemical properties: lower molecular weight and lower logPwhile maintaining potency (with a slight 2-fold improvement).