2. Academic Validation
  3. Aryloxy cyclohexyl imidazoles: a novel class of antileishmanial agents

Aryloxy cyclohexyl imidazoles: a novel class of antileishmanial agents

  • Bioorg Med Chem Lett. 2009 Jan 15;19(2):324-7. doi: 10.1016/j.bmcl.2008.11.094.
Nagarapu Srinivas 1,  Shraddha Palne,  Nishi,  Suman Gupta,  Kalpana Bhandari
Affiliations

Affiliation

  • 1 Medicinal and Process Chemistry Division, Central Drug Research Institute, M.G. Marg, Lucknow, UP 226001, India.
PMID: 19091566 DOI: 10.1016/j.bmcl.2008.11.094
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 IC(50) 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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