| Literature DB >> 21295472 |
Vijay K Marrapu1, Nagarapu Srinivas, Monika Mittal, Nishi Shakya, Suman Gupta, Kalpana Bhandari.
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.Entities:
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Year: 2011 PMID： 21295472 DOI： 10.1016/j.bmcl.2011.01.026
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823