Please use this identifier to cite or link to this item:
https://hdl.handle.net/2440/55847
Citations | ||
Scopus | Web of Science® | Altmetric |
---|---|---|
?
|
?
|
Type: | Journal article |
Title: | 2,4,5-Triphenylisothiazol-3(2H)-one 1,1-dioxides as inhibitors of human leukocyte elastase. |
Author: | Gutschow, M. Pietsch, M. Themann, A. Fahrig, J. Schulze, B. |
Citation: | Journal of Enzyme Inhibition and Medicinal Chemistry, 2005; 20(4):341-347 |
Publisher: | Informa Healthcare |
Issue Date: | 2005 |
ISSN: | 1475-6366 1475-6374 |
Statement of Responsibility: | Michael Gütschow, Markus Pietsch, Andrea Themann, Janine Fahrigand Bärbel Schulze |
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. |
DOI: | 10.1080/14756360500148783 |
Description (link): | http://informahealthcare.com/doi/abs/10.1080/14756360500148783?journalCode=enz |
Published version: | http://dx.doi.org/10.1080/14756360500148783 |
Appears in Collections: | Aurora harvest Chemistry publications |
Files in This Item:
There are no files associated with this item.
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.