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dc.contributorWichita State University. Department of Chemistryen_US
dc.contributor.authorLai, Zhongen_US
dc.contributor.authorGan, Xiangdongen_US
dc.contributor.authorWei, Liuqingen_US
dc.contributor.authorAlliston, Kevin R.en_US
dc.contributor.authorYu, Hongyien_US
dc.contributor.authorLi, Yue Heen_US
dc.contributor.authorGroutas, William C.en_US
dc.date.accessioned2012-02-06T17:16:57Z
dc.date.available2012-02-06T17:16:57Z
dc.date.issued2004-09-15en_US
dc.identifier15313222en_US
dc.identifier0372430en_US
dc.identifierS0003986104003327en_US
dc.identifierHL 57788en_US
dc.identifier.citationArchives of biochemistry and biophysics. 2004 Sep 15; 429(2): 191-7.en_US
dc.identifier.issn0003-9861en_US
dc.identifier.urihttp://dx.doi.org/10.1016/j.abb.2004.06.014en_US
dc.identifier.urihttp://hdl.handle.net/10057/4370
dc.descriptionClick on the DOI link below to access the article (may not be free).en_US
dc.description.abstractThe design, synthesis, and in vitro biochemical evaluation of a class of mechanism-based inhibitors of human leukocyte elastase (HLE) that incorporate in their structure a 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold with appropriate recognition and reactivity elements appended to it is described. The synthesized compounds were found to be efficient, time-dependent inhibitors of HLE. The interaction of the inhibitors with HLE is postulated to lead to the formation of a highly reactive N-sulfonyl imine (a Michael acceptor) that arises from an enzyme-induced sulfonamide fragmentation cascade. Subsequent reaction ultimately leads to the formation of a relatively stable acyl enzyme. The results cited herein demonstrate convincingly the superiority of the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold over other scaffolds (e.g., saccharin) in the design of inhibitors of (chymo)trypsin-like serine proteases.en_US
dc.description.sponsorshipNHLBI NIH HHSen_US
dc.format.extent191-7en_US
dc.language.isoengen_US
dc.publisherElsevieren_US
dc.relation.ispartofseriesArchives of biochemistry and biophysicsen_US
dc.relation.ispartofseriesArch. Biochem. Biophys.en_US
dc.sourceNLMen_US
dc.subjectResearch Support, Non-U.S. Gov'ten_US
dc.subjectResearch Support, U.S. Gov't, P.H.S.en_US
dc.subject.meshCyclic S-Oxides/chemistryen_US
dc.subject.meshEnzyme Inhibitors/chemistryen_US
dc.subject.meshHumansen_US
dc.subject.meshLeukocyte Elastase/antagonists & inhibitorsen_US
dc.subject.meshMagnetic Resonance Spectroscopyen_US
dc.subject.meshSulfonamides/chemistryen_US
dc.subject.meshThiazoles/chemistryen_US
dc.subject.meshEnzyme Inhibitors/pharmacologyen_US
dc.subject.meshSulfonamides/pharmacologyen_US
dc.titlePotent inhibition of human leukocyte elastase by 1,2,5-thiadiazolidin-3-one 1,1 dioxide-based sulfonamide derivativesen_US
dc.typeArticleen_US
dc.coverage.spacialUnited Statesen_US
dc.description.versionpeer revieweden_US
dc.rights.holderCopyright © 2004, Elsevieren_US


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