Literature DB >> 10866393

Synthesis and activity studies of conformationally restricted alpha-ketoamide factor Xa inhibitors.

J Cacciola1, J M Fevig, P F Stouten, R S Alexander, R M Knabb, R R Wexler.   

Abstract

Conformationally restricted borolysine compounds containing a 2-(2-cyanophenylthio) benzoyl in the P3 position unexpectedly led to enhanced factor Xa inhibition. In an effort to improve both the potency and selectivity of this series by extending into the S' domain, we have replaced the boronic acid with alpha-ketoamides, utilizing a novel process that was developed in our labs.

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Year:  2000        PMID: 10866393     DOI: 10.1016/s0960-894x(00)00215-8

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Convergent synthesis of alpha-ketoamide inhibitors of Pin1.

Authors:  Guoyan G Xu; Felicia A Etzkorn
Journal:  Org Lett       Date:  2010-02-19       Impact factor: 6.005

  1 in total

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