| Synthesis of some 5-phenylisoxazole-3-carboxylic acid derivatives as potent xanthine oxidase inhibitors. | |
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MedLine Citation:
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PMID: 20189693 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A number of 5-phenylisoxazole-3-carboxylic acid derivatives (5a-e, 11a-e) were synthesized and analyzed for their ability to inhibit xanthine oxidase. Most of the compounds exhibited potency levels in the micromolar/submicromolar range. The presence of a cyano group at the 3-position of phenyl moiety turned out to be the preferred substitution pattern, as its transformation into the nitro group determined a general reduction of the inhibitory potency. A molecular modeling study on compound 11a was performed to gain an insight into its binding mode with xanthine oxidase, and to provide the basis for further structure-guided design of new non-purine xanthine oxidase inhibitors related with 5-phenylisoxazole-3-carboxylic acid scaffold. |
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Authors:
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Shaojie Wang; Jufang Yan; Jian Wang; Jiarun Chen; Tingjian Zhang; Yong Zhao; Mingxing Xue |
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Publication Detail:
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Type: Journal Article Date: 2010-02-10 |
Journal Detail:
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Title: European journal of medicinal chemistry Volume: 45 ISSN: 1768-3254 ISO Abbreviation: Eur J Med Chem Publication Date: 2010 Jun |
Date Detail:
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Created Date: 2010-04-20 Completed Date: 2010-07-27 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0420510 Medline TA: Eur J Med Chem Country: France |
Other Details:
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Languages: eng Pagination: 2663-70 Citation Subset: IM |
Copyright Information:
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Copyright (c) 2010 Elsevier Masson SAS. All rights reserved. |
Affiliation:
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Key Laboratory of New Drugs Design and Discovery of Liaoning Province, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China. sjwang_99@yahoo.com.cn |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Carboxylic Acids / chemical synthesis*, chemistry, pharmacology* Cattle Enzyme Inhibitors / chemical synthesis*, chemistry, pharmacology* Humans Isoxazoles / chemical synthesis*, chemistry, pharmacology* Models, Molecular Molecular Conformation Structure-Activity Relationship Xanthine Oxidase / antagonists & inhibitors* |
| Chemical | |
Reg. No./Substance:
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0/5-phenylisoxazole-3-carboxylic acid; 0/Carboxylic Acids; 0/Enzyme Inhibitors; 0/Isoxazoles; EC 1.17.3.2/Xanthine Oxidase |
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