Bioorganic and Medicinal Chemistry Letters p. 3583 - 3588 (1998)
Update date:2022-08-03
Topics:
Ambler, John
Baker, Emma
Brown, Lyndon
Butler, Paul
Farr, Dave
Dunnet, Karen
Le Grand, Darren
Janus, Diana
Jones, Darryl
Menear, Keith
Mercer, Mark
Smith, Garrick
Talbot, Mark
Tweed, Morris
The chemical optimisation of CGH1668 1 is described employing an in vivo model of absorption to determine the influence on bioavailability of single point modifications to five key molecular templates. The discovery of an orally bioavailable and selective thrombin inhibitor, 24, highlights the utility of this approach.
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