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Silanediol-based inhibitor of thermolysin |
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| Authors: | Kim Jaeseung Glekas Athanasios McN Sieburth Scott |
| Affiliation: | a Department of Chemistry, State University of New York at Stony Brook, Stony Brook, NY 11794-3400, USA b Department of Chemistry, Temple University, 1901 N. 13th St, Philadelphia, PA 19122, USA |
| Abstract: | The first silanediol inhibitor of thermolysin is reported, prepared by analogy with the Grobelny/Bartlett phosphinate inhibitor. A Cbz group on nitrogen proved to be unstable to the triflic acid mediated silanediol deprotection and was replaced with a dihydrocinnamoyl group. The silanediol was prepared in high purity by hydrolysis of a difluorosilane intermediate and proved to be an effective inhibitor, differing from the phosphinate by a factor of 4 (Ki=41 nM). |
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