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Synthesis, evaluation, and crystallographic analysis of L-371,912: A potent and selective active-site thrombin inhibitor

✍ Scribed by Terry A. Lyle; Zhongguo Chen; Sandra D. Appleby; Roger M. Freidinger; Stephen J. Gardell; S.Dale Lewis; Ying Li; Elizabeth A. Lyle; Joseph J. Lynch Jr.; Anne M. Mulichak; Assunta S. Ng; Adel M. Naylor-Olsen; William M. Sanders

Publisher
Elsevier Science
Year
1997
Tongue
English
Weight
336 KB
Volume
7
Category
Article
ISSN
0960-894X

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✦ Synopsis

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 thrombin over related serine proteases and is efficacious in an animal model of arterial thrombosis.

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