Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 1, Pages 291-293Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.10.117
Keywords
Leishmania; Azoles; Imidazoles; Aryloxy cyclohexane
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Funding
- University Grants Commission (India)
- Council of Scientific and Industrial Research (India)
- SIP
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A series of aryloxy alkyl/aryl alkyl imidazoles were synthesized and evaluated in vitro as antileishmanials against Leishmania donovani. All the 19 compounds exhibited 94-100% inhibition at 10 mu g/mL against promastigotes and 12 compounds exhibited high inhibition with an IC50 in the range of 0.47-4.85 mu g/mL against amastigotes. Promising compounds were tested further in vivo. Among all, compounds 4 and 23 with 4-CF3 aryloxy moiety exhibited medium in vivo inhibition of 58-60%, thus providing new structural lead for antileishmanials. (c) 2009 Elsevier Ltd. All rights reserved.
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