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Merck

Thrombin inhibitors built on an azaphenylalanine scaffold.

Bioorganic & medicinal chemistry letters (2004-03-10)
Anamarija Zega, Gregor Mlinsek, Tomaz Solmajer, Alenka Trampus-Bakija, Mojca Stegnar, Uros Urleb
摘要

A series of azaphenylalanine derivatives were investigated as novel thrombin inhibitors based on the prodrug principle. By systematic structural modifications we have identified optimal groups for this series that led us to potent inhibitors of thrombin incorporating the benzamidine fragment at the P1 position, and their potentially orally active benzamidoxime prodrugs. The binding modes in the thrombin active site of two representative compounds were identified by X-ray crystallographic analysis.

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2-萘酚-6-磺酸 钠盐 水合物, technical grade