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https://hdl.handle.net/2440/55847
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DC Field | Value | Language |
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dc.contributor.author | Gutschow, M. | - |
dc.contributor.author | Pietsch, M. | - |
dc.contributor.author | Themann, A. | - |
dc.contributor.author | Fahrig, J. | - |
dc.contributor.author | Schulze, B. | - |
dc.date.issued | 2005 | - |
dc.identifier.citation | Journal of Enzyme Inhibition and Medicinal Chemistry, 2005; 20(4):341-347 | - |
dc.identifier.issn | 1475-6366 | - |
dc.identifier.issn | 1475-6374 | - |
dc.identifier.uri | http://hdl.handle.net/2440/55847 | - |
dc.description.abstract | A series of substituted 2,4,5-triphenylisothiazol-3(2H)-one 1,1-dioxides 9 was synthesized and investigated as inhibitors of human leukocyte elastase (HLE). All compounds were found to inhibit HLE in a time-dependent manner and most of them exhibited kobs/[I] values > 300 M− 1s− 1. The most potent 3-oxosultam of this series was 9l (kobs/[I] = 2440 M− 1s− 1). Kinetic investigations performed with 9g and different substrate concentrations did not allow to clearly distinguish between a competitive or noncompetitive mode of inhibition. A more complex interaction is supported by the failure of a linear dependency of kobs values on the inhibitor concentration. | - |
dc.description.statementofresponsibility | Michael Gütschow, Markus Pietsch, Andrea Themann, Janine Fahrigand Bärbel Schulze | - |
dc.description.uri | http://informahealthcare.com/doi/abs/10.1080/14756360500148783?journalCode=enz | - |
dc.language.iso | en | - |
dc.publisher | Informa Healthcare | - |
dc.source.uri | http://dx.doi.org/10.1080/14756360500148783 | - |
dc.title | 2,4,5-Triphenylisothiazol-3(2H)-one 1,1-dioxides as inhibitors of human leukocyte elastase. | - |
dc.type | Journal article | - |
dc.identifier.doi | 10.1080/14756360500148783 | - |
pubs.publication-status | Published | - |
Appears in Collections: | Aurora harvest Chemistry publications |
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