Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594037 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
A small library of 25 triazole/tetrazole-based sulfonamides have been synthesized and further evaluated for their inhibitory activity against thrombin, trypsin, tryptase and chymase. In general, the triazole-based sulfonamides inhibited thrombin more efficiently than the tetrazole counterparts. Particularly, compound 26 showed strong thrombin inhibition (Ki = 880 nM) and significant selectivity against other human related serine proteases like trypsin (Ki = 729 μM). Thrombin binding affinity of the same compound was determined by ITC and demonstrated that the binding of this new triazole-based scaffold is enthalpically driven, making it a good candidate for further development.
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Rogelio Siles, Yuko Kawasaki, Patrick Ross, Ernesto Freire,