2. Academic Validation
  3. Synthesis of substituted aryloxy alkyl and aryloxy aryl alkyl imidazoles as antileishmanial agents

Synthesis of substituted aryloxy alkyl and aryloxy aryl alkyl imidazoles as antileishmanial agents

  • Bioorg Med Chem Lett. 2010 Jan 1;20(1):291-3. doi: 10.1016/j.bmcl.2009.10.117.
Kalpana Bhandari 1,  Nagarapu Srinivas,  Vijay K Marrapu,  Aditya Verma,  Saumya Srivastava,  Suman Gupta
Affiliations

Affiliation

  • 1 Medicinal and Process Chemistry Division, Central Drug Research Institute, CSIR, Lucknow 226 001, India. kalpana_bhandari@cdri.res.in
PMID: 19913413 DOI: 10.1016/j.bmcl.2009.10.117
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 10microg/mL against promastigotes and 12 compounds exhibited high inhibition with an IC(50) in the range of 0.47-4.85microg/mL against amastigotes. Promising compounds were tested further in vivo. Among all, compounds 4 and 23 with 4-CF(3) aryloxy moiety exhibited medium in vivo inhibition of 58-60%, thus providing new structural lead for antileishmanials.

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