The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa

S D Jones; J W Liebeschuetz; P J Morgan; C W Murray; A D Rimmer; J M Roscoe; B Waszkowycz; P M Welsh; W A Wylie; S C Young; H Martin; J Mahler; L Brady; K Wilkinson

doi:10.1016/s0960-894x(01)00042-7

The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa

Bioorg Med Chem Lett. 2001 Mar 12;11(5):733-6. doi: 10.1016/s0960-894x(01)00042-7.

Authors

S D Jones¹, J W Liebeschuetz, P J Morgan, C W Murray, A D Rimmer, J M Roscoe, B Waszkowycz, P M Welsh, W A Wylie, S C Young, H Martin, J Mahler, L Brady, K Wilkinson

Affiliation

¹ Prosthetics Molecular Design, Beechfield House, Macclesfield, UK. stuart.jones@protherics.com

PMID: 11266180
DOI: 10.1016/s0960-894x(01)00042-7

Abstract

Factor Xa, a critical serine protease in the blood coagulation cascade, has become a target for inhibition as a strategy for the invention of novel anti-thrombotic agents. Here we describe the development of phenylglycine containing benzamidine carboxamides as novel, potent and selective inhibitors of factor Xa.

MeSH terms

Benzamidines / chemistry*
Benzamidines / pharmacology
Binding Sites
Combinatorial Chemistry Techniques
Crystallography, X-Ray
Drug Design
Factor Xa / metabolism
Factor Xa Inhibitors*
Glycine / analogs & derivatives
Glycine / chemistry*
Glycine / pharmacology*
Models, Molecular
Molecular Structure
Protein Structure, Tertiary
Software

Substances

Benzamidines
Factor Xa Inhibitors
2-phenylglycine
Factor Xa
Glycine