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dc.contributorWichita State University. Department of Chemistryen_US
dc.contributor.authorGroutas, William C.en_US
dc.contributor.authorBrubaker, Michael J.en_US
dc.contributor.authorChong, Lee S.en_US
dc.contributor.authorEpp, Jeffrey B.en_US
dc.contributor.authorHuang, Heen_US
dc.contributor.authorKeller, C. E.en_US
dc.contributor.authorMcClenahan, Jerry J.en_US
dc.contributor.authorGivens, R. S.en_US
dc.contributor.authorSingh, R.en_US
dc.contributor.authorZandler, Melvin E.en_US
dc.date.accessioned2012-02-06T17:17:26Z
dc.date.available2012-02-06T17:17:26Z
dc.date.issued1994-02-01en_US
dc.identifier8075302en_US
dc.identifier9200627en_US
dc.identifierHL 38048en_US
dc.identifier.citationDrug design and discovery. 1994 Feb; 11(2): 149-57.en_US
dc.identifier.issn1055-9612en_US
dc.identifier.issn1026-7921en_US
dc.identifier.urihttp://hdl.handle.net/10057/4422
dc.descriptionFull text of this article is not available in SOAR.en_US
dc.description.abstractA structure-activity relationship study was conducted in order to probe the nature of the interaction between some 3-alkyl-N-hydroxysuccinimide derivatives and human leukocyte elastase. The structural features in substituent X (structure I) that lead to the manifestation and optimization of inhibitory activity have been examined. The data suggest that the presence of an alkyl or aryl(sulfonyloxy) group in the active compounds may serve a triple purpose, namely, it functions as a good leaving group as dictated by the established mechanism of action of this class of compounds, secondly, it may enhance binding by assuming a favorable spatial orientation and, thirdly, it may increase the chemical reactivity of the carbonyl carbon in the bioactive compounds.en_US
dc.description.sponsorshipNHLBI NIH HHSen_US
dc.format.extent149-57en_US
dc.language.isoengen_US
dc.publisherHarwood Academic Publishersen_US
dc.relation.ispartofseriesDrug design and discoveryen_US
dc.relation.ispartofseriesDrug Des Discoven_US
dc.sourceNLMen_US
dc.subjectResearch Support, U.S. Gov't, P.H.S.en_US
dc.subject.lcshLeukocyte Elastase/chemistryen_US
dc.subject.lcshPancreatic Elastase/chemistryen_US
dc.subject.lcshSuccinimides/pharmacologyen_US
dc.subject.meshChemistry, Physicalen_US
dc.subject.meshCrystallography, X-Rayen_US
dc.subject.meshHumansen_US
dc.subject.meshLeukocyte Elastase/antagonists & inhibitorsen_US
dc.subject.meshLeukocytes/enzymologyen_US
dc.subject.meshMagnetic Resonance Spectroscopyen_US
dc.subject.meshPancreatic Elastase/antagonists & inhibitorsen_US
dc.subject.meshPhysicochemical Phenomenaen_US
dc.subject.meshStructure-Activity Relationshipen_US
dc.subject.meshSuccinimides/chemistryen_US
dc.titleDerivatives of 3-alkyl-N-hydroxysuccinimide: probing the effect of structure on bioactivity toward human leukocyte elastaseen_US
dc.typeArticleen_US
dc.coverage.spacialSwitzerlanden_US
dc.description.versionpeer revieweden_US
dc.rights.holderCopyright © 1994 Harwood Academic Publishersen_US


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