Novel bicyclic lactam inhibitors of thrombin: highly potent and selective inhibitors

Bioorganic & Medicinal Chemistry Letters
Yves St-DenisM Arshad Siddiqui

Abstract

The potency and selectivity of a previous series of low molecular weight thrombin inhibitors were improved through modifications of the P1 and P3 residues. Introduction of diphenyl substituted sulfonamides in the P3 moiety led to highly efficacious compounds. By correctly selecting the combination of P1 and P3 residues, high levels of potency, selectivity and in vivo efficacy were obtained.

References

Jun 1, 1973·The Journal of Organic Chemistry·W NagaiL A Cohen
Apr 15, 1994·Journal of Medicinal Chemistry·T NagaharaM Iwamoto
Jan 5, 1999·Bioorganic & Medicinal Chemistry Letters·Y St-DenisM A Siddiqui
Nov 27, 2001·Bioorganic & Medicinal Chemistry Letters·S LévesqueM A Siddiqui

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Citations

Jan 5, 1999·Bioorganic & Medicinal Chemistry Letters·Y St-DenisM A Siddiqui
May 14, 2014·Journal of Biomolecular Structure & Dynamics·Divya Gopalakrishnan NairSadasivan Chittalakkottu
Nov 9, 2005·Bioorganic & Medicinal Chemistry Letters·Ian ChurcherJonathan D J Wrigley

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