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 |
Date Deposited | 17 Oct 2011 14:47 |
ORCID: https://orcid.org/0009-0005-3744-7003