Tetrahydronaphthyl azole oxime ethers: the conformationally rigid analogues of oxiconazole as antibacterials
IR@CDRI: CSIR-Central Drug Research Institute, Lucknow
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| Creator |
Bhandari, Kalpana
Srinivas, Nagarapu Keshva, G B S Shukla, P K |
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| Date |
2010-09-09T08:52:58Z
2010-09-09T08:52:58Z 2009 |
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| Identifier |
European Journal of Medicinal Chemistry, 44, 1, 2009, 437-447
http://hdl.handle.net/123456789/591 |
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| Description |
A series of novel (Z)- and (E)-2-imidazolo-/triazolo-methyl tetrahydronaphthyl oxime ethers (7-28) were synthesized as conformationally constrained analogues of oxiconazole and evaluated for antifungal and antibacterial activities. Many of these derivatives exhibited potent antibacterial activity and surprisingly none of them was active against fungal strains. The SAR studies showed that imidazole oxime ethers were more active than the corresponding triazole oxime ethers. Imidazole derivatives 8, 11, 12, 15, 18, 19, 21 and 23 exhibited high inhibitory activity with 1.56–0.39 µg/mL MIC values against Klebsiella pneumoniae, Escherichia coli and Staphylococus aureus. These compounds represent new structure scaffolds that can be further optimized to give new antibacterial agents with structures significantly different from those of existing classes of antibiotics.
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234556 bytes
application/pdf |
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| Language |
en
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| Subject |
Oxiconazole
Antimicrobials Rigid analogues Tetrahydronaphthyl oxime ethers Antibacterial activity |
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| Title |
Tetrahydronaphthyl azole oxime ethers: the conformationally rigid analogues of oxiconazole as antibacterials
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| Type |
Article
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