Design and synthesis of novel tetrahydronaphthyl azoles and related cyclohexyl azoles as antileishmanial agents

  • Bioorg Med Chem Lett. 2011 Mar 1;21(5):1407-10. doi: 10.1016/j.bmcl.2011.01.026.
Vijay K Marrapu  1 ,  Nagarapu Srinivas ,  Monika Mittal ,  Nishi Shakya ,  Suman Gupta ,  Kalpana Bhandari
Affiliations
  • 1. Medicinal and Process Chemistry Division, Central Drug Research Institute, CSIR, Lucknow, India.
PMID: 21295472 DOI: 10.1016/j.bmcl.2011.01.026
Abstract

A novel series of trans-2-aryloxy-1,2,3,4,-tetrahydronaphthyl azoles and related cyclohexyl azoles were synthesized and evaluated in vitro against Leishmania donovani. Compound 9 identified as most active analog with IC(50) value of 0.64 μg/mL and SI value of 34.78 against amastigotes, and is several folds more potent than the reference drugs sodium stilbogluconate and paromomycin. It also exhibited significant in vivo inhibition of 83.33%, and provided a new structural scaffold for antileishmanials.