2. Academic Validation
  3. Design and synthesis of novel tetrahydronaphthyl azoles and related cyclohexyl azoles as antileishmanial agents

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

Affiliation

  • 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.

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