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
  • 1. Medicinal and Process Chemistry Division, Central Drug Research Institute, CSIR, Lucknow 226 001, India. [email protected]
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.