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

Yang, Mei; Arai, Chika; Bakar Md, Abu; Lu, Jun; Ge, Jian-Feng; Pudhom, Khanitha; Takasu, Kiyosei; Kasai, Kazuki; Kaiser, Marcel; Brun, Reto; +3 more...Yardley, VanessaORCID logo; Itoh, Isamu; and Ihara, Masataka (2010) Fluorinated rhodacyanine (SJL-01) possessing high efficacy for visceral leishmaniasis (VL). Journal of medicinal chemistry, 53 (1). pp. 368-373. ISSN 0022-2623 DOI: 10.1021/jm9013086
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Anti-Leishmania in vitro and in vivo activities of various rhodacyanine derivatives have been examined. Among them, the fluorinatied variant SJL-01 (8) showed IC(50) of 0.011 microM 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 x 5 iv administrations. Negative results on chromosomal aberration test and in vitro micronucleus test suggest that compound 8 is a hopeful candidate for visceral leishmaniasis (VL).

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