Fluorinated rhodacyanine (SJL-01) possessing high efficacy for visceral leishmaniasis (VL)

…, K Pudhom, K Takasu, K Kasai, M Kaiser…

文献索引：Yang, Mei; Arai, Chika; Bakar Md., Abu; Lu, Jun; Ge, Jian-Feng; Pudhom, Khanitha; Takasu, Kiyosei; Kasai, Kazuki; Kaiser, Marcel; Brun, Reto; Yardley, Vanessa; Itoh, Isamu; Ihara, Masataka Journal of Medicinal Chemistry, 2010 , vol. 53, # 1 p. 368 - 373

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被引用次数: 21

摘要

Anti-Leishmania in vitro and in vivo activities of various rhodacyanine derivatives have been examined. Among them, the fluorinatied variant SJL-01 (8) showed IC50 of 0.011 μM against Leishmania donovani strain MHOM/ET/67/L82 (selective index of> 15000) and 95− 97% inhibition against L. donovani strain MHOM/ET/67/HU in female BALB/c mice by 1.3− 12.5 mg/kg× 5 iv administrations. Negative results on chromosomal aberration test and in ...