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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Authors | Mei Yang, 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 |
Journal | Journal of medicinal chemistry
(J Med Chem)
Vol. 53
Issue 1
Pg. 368-73
(Jan 14 2010)
ISSN: 1520-4804 [Electronic] United States |
PMID | 19894726
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- 2-((3-ethyl-5-(2-(3-methylbenzo(d)thiazol-2(3H)-ylidene)ethylidene)-4-oxothiazolidin-2-ylidene)methyl)-5-fluoro-3-methylbenzo(d)thiazol-3-ium
- Antiprotozoal Agents
- Benzothiazoles
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Topics |
- Animals
- Antiprotozoal Agents
(chemistry, pharmacology)
- Benzothiazoles
(chemistry, pharmacology)
- Cell Line
- Cell Survival
(drug effects)
- Female
- Leishmania donovani
(drug effects)
- Leishmaniasis, Visceral
(drug therapy)
- Macrophages
(drug effects)
- Mice
- Mice, Inbred BALB C
- Parasitic Sensitivity Tests
- Rats
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