Synthesis of substituted aryloxy alkyl and aryloxy aryl alkyl imidazoles as antileishmanial agents |
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Authors: | Kalpana Bhandari Nagarapu Srinivas Vijay K Marrapu Aditya Verma Saumya Srivastava Suman Gupta |
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Institution: | 1. Medicinal and Process Chemistry Division, Central Drug Research Institute, CSIR, Lucknow 226 001, India;2. Division of Parasitology, Central Drug Research Institute, CSIR, Lucknow 226 001, India |
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Abstract: | 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 μg/mL against promastigotes and 12 compounds exhibited high inhibition with an IC50 in the range of 0.47–4.85 μg/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. |
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