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Bioorg Med Chem Lett. 1998 Dec 15;8(24):3583-8.

The discovery of orally available thrombin inhibitors: studies towards the optimisation of CGH1668.

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1
Novartis Horsham Research Center, West Sussex.

Abstract

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.

PMID:
9934475
DOI:
10.1016/s0960-894x(98)00640-4
[Indexed for MEDLINE]

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