Aryloxy cyclohexyl imidazoles: A novel class of antileishmanial agents |
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| Authors: | Nagarapu Srinivas Shraddha Palne Suman Gupta Kalpana Bhandari |
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| Institution: | 1. Medicinal and Process Chemistry Division, Central Drug Research Institute, M.G. Marg, Lucknow, U.P. 226001, India;2. Division of Parasitology, Central Drug Research Institute, Lucknow 226001, India |
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| Abstract: | Thirteen novel aryloxy cyclohexane-based mono and bis imidazoles were synthesized and evaluated in vitro as antileishmanials against Leishmania donovani and cytotoxicity assessed. These compounds were better than the existing drugs, sodium stibogluconate and pentamidine in respect to IC50 and SI values. Promising compounds were tested further in vivo. Among all, the bis methylimidazole with 2-fluoro, 4-nitro aryloxy group (9) exhibited significant in vivo inhibition of 77.9%, thus providing new structural lead for antileishmanials. |
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