Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 North Charles Street, Baltimore, Maryland 21218-2685, United States.
J Med Chem. 2012 Jan 12;55(1):291-6. doi: 10.1021/jm201214d. Epub 2011 Dec 15.
Sixteen new anilide derivatives of the natural trioxane artemisinin were prepared and evaluated for antimalarial efficacy in Plasmodium berghei infected mice. Of these 16 new anilides administered orally as one 6 mg/kg dose combined with 18 mg/kg mefloquine hydrochloride, only sulfide 3-arteSanilide 12d was completely curative: on day 30 after infection, all mice in this group had no detectable parasitemia, gained as much weight as the uninfected control mice, and behaved normally.
十六个新的天然三氧烷青蒿素的酰苯胺衍生物被制备并评估其在感染伯氏疟原虫的小鼠中的抗疟功效。在这些新的酰苯胺中,只有 3-磺胺基-12d 在口服给予 6mg/kg 剂量与 18mg/kg 盐酸甲氟喹联合用药时具有完全的治愈效果:在感染后 30 天,该组的所有小鼠均未检测到寄生虫血症,体重增加与未感染的对照小鼠相同,且行为正常。