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The discovery of orally available thrombin inhibitors: optimisation of the P1 pharmacophore. 1999
J Ambler, and
D Bentley, and
L Brown, and
K Dunnet, and
D Farr, and
D Janus, and
D Le Grand, and
K Menear, and
M Mercer, and
M Talbot, and
M Tweed, and
B Wathey
Novartis Horsham Research Centre, Horsham, West Sussex.
Thrombin inhibitors have been designed with the replacement of the strongly basic guanidine P1 pharmocophore with a group that exploits the lipophilicity of the S1 pocket. The approach has lead to the discovery of potent thrombin inhibitors demonstrating good intra-duodenal absorption.
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