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

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).
AuthorsMei 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
JournalJournal of medicinal chemistry (J Med Chem) Vol. 53 Issue 1 Pg. 368-73 (Jan 14 2010) ISSN: 1520-4804 [Electronic] United States
PMID19894726 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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
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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