P3 optimization of functional potency, in vivo efficacy and oral bioavailability in 3-aminopyrazinone thrombin inhibitors bearing non-charged groups at the P1 position

Richard C.A. Isaacs,Christina L. Newton,Kellie J. Cutrona,Swati P. Mercer,Bruce D. Dorsey,Colleen M. McDonough,Jacquelynn J. Cook,Julie A. Krueger,S. Dale Lewis,Bobby J. Lucas,Elizabeth A. Lyle,Joseph J. Lynch,Cynthia Miller-Stein,Maria T. Michener,Audrey A. Wallace,Rebecca B. White,Bradley K. Wong

Bioorganic & Medicinal Chemistry Letters（2011）

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摘要

A series of 3-aminopyrazinone P2 thrombin inhibitors bearing non-charged groups (X, Y) at the P1 benzylamino position was optimized with respect to functional potency, in vivo efficacy and oral bioavailability by manipulation of polarity at the P3 pyridine position (Z=H, piperidine; Z=O, pyridine-N-oxide).

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关键词

Thrombin,Inhibitor,Coagulation,Efficacy

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