Tripeptidyl pyridinium methyl ketones as potent active site inhibitors of thrombin
โ Scribed by Torsten Steinmetzer; Yasuo Konishi
- Book ID
- 103983462
- Publisher
- Elsevier Science
- Year
- 1996
- Tongue
- English
- Weight
- 295 KB
- Volume
- 6
- Category
- Article
- ISSN
- 0960-894X
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๐ SIMILAR VOLUMES
Removal of the [3-ketoamide functionality from L-370,518 (K~ = 0.09 nM) provided a 5 nM K i inhibitor of thrombin: L-371,912. Comparison of the enzyme-inhibitor crystal structures suggests a possible explanation for the relatively small change in affinity for thrombin. L-371,912 is selective for thr
Synthesis, Evaluation, and Crystallographic Analysis of L-371,912: A Potent and Selective Active-Site Thrombin Inhibitor. -Two major synthetic challenges are apparent in more efficient approaches to the synthesis of the novel trans 4-aminocyclohexylglycine ketoamide found in inhibitor (IX). The firs