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ID: ALA1681663

Journal: Bioorg Med Chem Lett

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

Authors: Marrapu VK, Srinivas N, Mittal M, Shakya N, Gupta S, Bhandari K.

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.

CiteXplore: 21295472

DOI: 10.1016/j.bmcl.2011.01.026