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JOURNAL OF MEDICINAL CHEMISTRY
Volume 53, Issue 1, Pages 368-373Publisher
AMER CHEMICAL SOC
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 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).
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