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High-throughput synthesis and optimization of thrombin inhibitors via urazole alpha-addition and Michael addition
P Douglas Boatman1, Jan Urban, Minh Nguyen
1Molecumetics, 2023 120th Ave NE, Bellevue, WA 98005, USA. dboatman@arenapharm.com
Bioorganic & Medicinal Chemistry Letters
|April 2, 2003
Abstract:
A novel alpha-addition of propiolates to urazoles followed by Michael addition of a variety of nucleophiles has been developed for rapid production and optimization of peptidomimetic drug leads. This technology has produced a number of highly potent and selective inhibitors of the serine protease, thrombin.