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