Studies towards the identification of potent, selective and bioavailable thrombin inhibitors

J Ambler; E Baker; D Bentley; L Brown; K Butler; P Butler; D Farr; K Dunnet; D Le Grand; J Hayler; D Janus; D Jones; K Menear; M Mercer; G Smith; M Talbot; M Tweed

doi:10.1016/s0960-894x(99)00061-x

Studies towards the identification of potent, selective and bioavailable thrombin inhibitors

Bioorg Med Chem Lett. 1999 Mar 8;9(5):737-42. doi: 10.1016/s0960-894x(99)00061-x.

Authors

J Ambler¹, E Baker, D Bentley, L Brown, K Butler, P Butler, D Farr, K Dunnet, D Le Grand, J Hayler, D Janus, D Jones, K Menear, M Mercer, G Smith, M Talbot, M Tweed

Affiliation

¹ Novartis Horsham Research Center, West Sussex.

PMID: 10201839
DOI: 10.1016/s0960-894x(99)00061-x

Abstract

The application of selection criteria, based on potency and physicochemical parameters, to a candidate library of thrombin inhibitors is described. The utility of the approach is exemplified by the discovery of a potent, selective and bioavailable thrombin inhibitor 62.

MeSH terms

Anticoagulants / isolation & purification
Anticoagulants / pharmacokinetics
Anticoagulants / pharmacology*
Biological Availability
Structure-Activity Relationship
Thrombin / antagonists & inhibitors*

Substances

Anticoagulants
Thrombin