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

IR@CDRI: CSIR-Central Drug Research Institute, Lucknow

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Field Value
 
Creator Marrapu, V K
Srinivas, Nagarapu
Mittal, Monika
Shakya, Nishi
Gupta, Suman
Bhandari, Kalpana
 
Date 2011-03-21T11:29:34Z
2011-03-21T11:29:34Z
2011
 
Identifier Bioorganic & Medicinal Chemistry Letters 21 (2011) 1407-1410
http://hdl.handle.net/123456789/657
 
Description : 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 IC50 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.
 
Format 235981 bytes
application/pdf
 
Language en
 
Relation CDRI Communication No 8015
 
Subject Antileishmanial
Azoles
Aryloxy tetrahydronaphthalene
 
Title Design and synthesis of novel tetrahydronaphthyl azoles and related cyclohexyl azoles as antileishmanial agents
 
Type Article