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

J Med Chem. 2010 Jan 14;53(1):368-73. doi: 10.1021/jm9013086.

Mei Yang ¹, Chika Arai, Abu Bakar Md, Jun Lu, Jian-Feng Ge, Khanitha Pudhom, Kiyosei Takasu, Kazuki Kasai, Marcel Kaiser, Reto Brun, Vanessa Yardley, Isamu Itoh, Masataka Ihara

Affiliations

Affiliation

1 Drug Discovery Science Research Center, Hoshi University, 2-4-41 Ebara, Shinagawa, Tokyo 142-8501, Japan.

PMID: 19894726 DOI: 10.1021/jm9013086

Abstract

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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