Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3, 3-disubstituted propionic acid derivatives in the P3 position

…, SD Lewis, SJ Gardell, BJ Lucas, JT Sisko…

Index: Tucker, Thomas J.; Lumma, William C.; Dale Lewis; Gardell, Stephen J.; Lucas, Bobby J.; Sisko, Jack T.; Lynch, Joseph J.; Lyle, Elizabeth A.; Baskin, Elizabeth P.; Woltmann, Richard F.; Appleby, Sandra D.; Chen, I.-Wu; Dancheck, Kimberley B.; Naylor-Olsen, Adel M.; Krueger, Julie A.; Cooper, Carolyn M.; Vacca, Joseph P. Journal of Medicinal Chemistry, 1997 , vol. 40, # 22 p. 3687 - 3693

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Citation Number: 31

Abstract

As part of an effort to prepare efficacious and orally bioavailable analogs of the previously reported thrombin inhibitors 1a, b, we have synthesized a series of compounds that utilize 3, 3-disubstituted propionic acid derivatives as P3 ligands. By removing the N-terminal amino group, the general oral bioavailability of this class of compounds was enhanced without excessively increasing the lipophilicity of the compounds. The overall properties of the ...

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[Beylin, V. G.; Chen, Huai G.; Dunbar, J.; Goel, O. P.; Harter, W.; et al. Tetrahedron Letters, 1993 , vol. 34, # 6 p. 953 - 956]

Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3, 3-disubstituted propionic acid derivatives in the P3 position

Abstract

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