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ChemInform Abstract: Synthesis, Evaluation, and Crystallographic Analysis of L-371,912: A Potent and Selective Active-Site Thrombin Inhibitor.

โœ Scribed by T. A. LYLE; Z. CHEN; S. D. APPLEBY; R. M. FREIDINGER; S. J. GARDELL; S. D. LEWIS; Y. LI; E. A. LYLE; J. J. JUN. LYNCH; A. M. MULICHAK; A. S. NG; A. M. NAYLOR-OLSEN; W. M. SANDERS

Publisher
John Wiley and Sons
Year
2010
Weight
36 KB
Volume
28
Category
Article
ISSN
0931-7597

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โœฆ Synopsis

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 first is the trans position of the groups on the cyclohexyl ring, and the second is the creation of the ฮฑ-ketoamide functionality. The improved synthetic route to (IX) makes it possible to synthesize the title compound (X). Compound (X) is selective for thrombin over related serine proteases and is efficacious in an animal model of arterial thrombosis. -(LYLE, T. A.; CHEN, Z.; APPLEBY,

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