Fluorinated Rhodacyanine (SJL-01) Possessing High Efficacy for Visceral Leishmaniasis (VL)

Yang, M; Arai, C; Md, AB; Lu, J; Ge, JF; Pudhom, K; Takasu, K; Kasai, K; Kaiser, M; Brun, R; Yardley, V; Itoh, I; Ihara, M; (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: https://doi.org/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 IC50 OfO-01 I PM against Lcishniania (Ionovani strain MHOM/ET/67/1_82 (selective index of > 15000) and 95-97% inhibition against L. clonovani strain MHOM/ET/67/HIJ in fernale BALB/c mice by 1.3-12.5 mg/kg x 5 iv administrations. Negative results on chromosonial aberration test and in vitro micronucleus test Suggest that compound 8 is a hopeful candidate for visceral leislinianiasis (VIL).

Item Type: Article
Keywords: in-vitro, dyes
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Immunology and Infection
Research Centre: Leishmaniasis Group
PubMed ID: 19894726
Web of Science ID: 273268300031
URI: http://researchonline.lshtm.ac.uk/id/eprint/4223


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