Fluorinated rhodacyanine (SJL-01) possessing high efficacy for visceral leishmaniasis (VL).
Mei Yang;
Chika Arai;
Abu Bakar Md;
Jun Lu;
Jian-Feng Ge;
Khanitha Pudhom;
Kiyosei Takasu;
Kazuki Kasai;
Marcel Kaiser;
Reto Brun;
+3 more...
Vanessa Yardley;
Isamu Itoh;
Masataka Ihara;
(2010)
Fluorinated rhodacyanine (SJL-01) possessing high efficacy for visceral leishmaniasis (VL).
Journal of medicinal chemistry, 53 (1).
pp. 368-373.
ISSN 0022-2623
DOI: 10.1021/jm9013086
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).
| Item Type | Article |
|---|---|
| Keywords | in-vitro, dyes |
| ISI | 273268300031 |