Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position

Kenneth E. Rittle,James C. Barrow,Kellie J. Cutrona,Kristen L. Glass,Julie A. Krueger,Lawrence C. Kuo,S.Dale Lewis,Bobby J. Lucas,Daniel R. McMasters,Matthew M. Morrissette,Philippe G. Nantermet,Christina L. Newton,William M. Sanders,Youwei Yan,Joseph P. Vacca,Harold G. Selnick

Bioorganic & Medicinal Chemistry Letters（2004）

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摘要

Thrombin inhibitors incorporating o-aminoalkylbenzylamides in the P1 position were designed, synthesized and found to have enhanced potency and selectivity in several different structural classes. X-ray crystallographic analysis of compound 24 bound in the α-thrombin–hirugen complex provides an explanation for these unanticipated results.

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