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https://hdl.handle.net/2440/55921
Type: | Journal article |
Title: | Synthesis of 2-phenylisothiazol-3(2H)-one 1,1 dioxides: inhibitors of human leukocyte elastase. |
Author: | Gutschow, M. Pietsch, M. Taubert, K. Freysoldt, T. Schulze, B. |
Citation: | Zeitschrift fuer Naturforschung, Section B: A Journal of Chemical Sciences, 2003; 58b:111-120 |
Publisher: | Verlag Z Naturforsch |
Issue Date: | 2003 |
ISSN: | 0932-0776 |
Statement of Responsibility: | Michael Gutschow, Markus Pietsch, Kathleen Taubert, Tonia H. E. Freysoldt, and Barbel Schulze |
Abstract: | A series of 2-phenylisothiazol-3(2H)-one 1,1-dioxides 14a – q were synthesized by oxidation of isothiazolium perchlorates 12. The inhibition of the serine proteases cathepsin G, chymotrypsin and human leukocyte elastase (HLE) by 14 was investigated. Some 4,5-diphenyl substituted derivatives ( 14i – k) were found to inhibit HLE in a time-dependent manner and exhibited kobs/[I] values > 500 M−1s−1. 14k (kobs/[I] = 2400 M−1s−1), was the most potent HLE inhibitor of this series. Kinetic investigations led to the conclusion that 2-phenylisothiazol-3(2H)-one 1,1-dioxides interact with HLE at the active site as well as at another binding site, resulting in a complex type of inhibition. |
Keywords: | Sultams Human Leukocyte Elastase Enzyme Inhibition |
Description (link): | http://www.znaturforsch.com/ab/v58b/c58b.htm |
Appears in Collections: | Aurora harvest 5 Chemistry publications |
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