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Utilization of the 1,2,3,5-thiatriazolidin-3-one 1,1-dioxide scaffold in the design of potential inhibitors of human neutrophil proteinase 3

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dc.contributor Wichita State University. Department of Chemistry en_US
dc.contributor.author Dou, Dengfeng en_US
dc.contributor.author He, Guijia en_US
dc.contributor.author Li, Yi en_US
dc.contributor.author Lai, Zhong en_US
dc.contributor.author Wei, Liuqing en_US
dc.contributor.author Alliston, Kevin R. en_US
dc.contributor.author Lushington, Gerald H. en_US
dc.contributor.author Eichhorn, David M. en_US
dc.contributor.author Groutas, William C. en_US
dc.date.accessioned 2012-02-06T17:17:22Z
dc.date.available 2012-02-06T17:17:22Z
dc.date.issued 2010-02-01 en_US
dc.identifier 20061159 en_US
dc.identifier 9413298 en_US
dc.identifier S0968-0896(09)01149-3 en_US
dc.identifier HL 57788/ R01 HL057788-08 en_US
dc.identifier.citation Bioorganic & medicinal chemistry. 2010 Feb; 18(3): 1093-102. en_US
dc.identifier.issn 1464-3391 en_US
dc.identifier.issn 0968-0896 en_US
dc.identifier.uri http://dx.doi.org/10.1016/j.bmc.2009.12.057 en_US
dc.identifier.uri http://hdl.handle.net/10057/4416
dc.description Click on the DOI link below to access the article (may not be free) en_US
dc.description.abstract The S' subsites of human neutrophil proteinase 3 (Pr 3) were probed by constructing diverse libraries of compounds based on the 1,2,3,5-thiatriazolidin-3-one 1,1-dioxide using combinational and click chemistry methods. The multiple points of diversity embodied in the heterocyclic scaffold render it well-suited to the exploration of the S' subsites of Pr 3. Molecular modeling studies suggest that further exploration of the S' subsites of Pr 3 using the aforementioned heterocyclic scaffold may lead to the identification of highly selective, reversible competitive inhibitors of Pr 3. en_US
dc.description.sponsorship NHLBI NIH HHS/ NHLBI NIH HHS en_US
dc.format.extent 1093-102 en_US
dc.language.iso eng en_US
dc.publisher Elsevier en_US
dc.relation.ispartofseries Bioorganic & medicinal chemistry en_US
dc.relation.ispartofseries Bioorg. Med. Chem. en_US
dc.source NLM en_US
dc.subject Research Support, N.I.H., Extramural en_US
dc.subject.mesh Crystallography, X-Ray en_US
dc.subject.mesh Humans en_US
dc.subject.mesh Models, Molecular en_US
dc.subject.mesh Myeloblastin/antagonists & inhibitors en_US
dc.subject.mesh Protein Binding en_US
dc.subject.mesh Serine Proteinase Inhibitors/chemistry* en_US
dc.subject.mesh Triazoles/chemistry en_US
dc.subject.mesh Myeloblastin/chemistry en_US
dc.subject.mesh Myeloblastin/metabolism en_US
dc.subject.mesh Serine Proteinase Inhibitors/pharmacology en_US
dc.subject.mesh Serine Proteinase Inhibitors/pharmacology en_US
dc.subject.mesh Triazoles/pharmacology en_US
dc.title Utilization of the 1,2,3,5-thiatriazolidin-3-one 1,1-dioxide scaffold in the design of potential inhibitors of human neutrophil proteinase 3 en_US
dc.type Article en_US
dc.coverage.spacial England en_US
dc.description.version peer reviewed en_US
dc.rights.holder Copyright © 2010, Elsevier en_US

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