mkt-077 and Leishmaniasis--Visceral

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).

Topics: Animals; Antiprotozoal Agents; Benzothiazoles; Cell Line; Cell Survival; Female; Leishmania donovani; Leishmaniasis, Visceral; Macrophages; Mice; Mice, Inbred BALB C; Parasitic Sensitivity Tests; Rats