烷基连接的双THTT衍生物作为有效的体外杀锥虫剂。
Alkyl-linked bis-THTT derivatives as potent in vitro trypanocidal agents.
作者信息
Coro Julieta, Atherton Richard, Little Susan, Wharton Hayley, Yardley Vanessa, Alvarez Amaury, Súarez Margarita, Pérez Rolando, Rodríguez Hortensia
机构信息
Laboratorio de Síntesis Orgánica, Facultad de Química, Universidad de la Habana, 10400-Ciudad Habana, Cuba.
出版信息
Bioorg Med Chem Lett. 2006 Mar 1;16(5):1312-5. doi: 10.1016/j.bmcl.2005.11.060. Epub 2005 Dec 15.
The effect of several alkyl-linked bis tetrahydro-(2H)-1,3,5-thiadiazine-2-thione (bis-THTT) on Leishmania donovani, Trypanosoma brucei rhodesiense, and Plasmodium falciparum is reported. Most of the compounds exhibited a potent activity against the three parasitic strains but the best in vitro activity profiles were found against T. b. rhodesiense with IC(50) values ranging between 0.3 and 4 microM for the most active compounds.
报道了几种烷基连接的双四氢-(2H)-1,3,5-噻二嗪-2-硫酮（双-THTT）对杜氏利什曼原虫、布氏罗得西亚锥虫和恶性疟原虫的作用。大多数化合物对这三种寄生虫菌株均表现出强效活性，但对布氏罗得西亚锥虫的体外活性最强，最具活性的化合物的半数抑制浓度（IC50）值在0.3至4微摩尔之间。
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