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

DOI: 10.1016/S0960-894X(98)00640-4

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 3583 - 3588 (1998)

Update date:2022-08-03

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Authors:

Ambler, JohnAmbler, John

Baker, EmmaBaker, Emma

Brown, LyndonBrown, Lyndon

Butler, PaulButler, Paul

Farr, DaveFarr, Dave

Dunnet, KarenDunnet, Karen

Le Grand, DarrenLe Grand, Darren

Janus, DianaJanus, Diana

Jones, DarrylJones, Darryl

Menear, KeithMenear, Keith

Mercer, MarkMercer, Mark

Smith, GarrickSmith, Garrick

Talbot, MarkTalbot, Mark

Tweed, MorrisTweed, Morris

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Article abstract of DOI:10.1016/S0960-894X(98)00640-4

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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Full text of DOI:10.1016/S0960-894X(98)00640-4

Products guided by the article

Product name:N-[2-(4-Aminophenyl)-1(S)-[4-(2-fluoroethyl)piperidin-1-ylcarbonyl]ethyl]-4-[1(S)-benzyl-2-(4-morpholinyl)ethyl]pyridine-3-sulfonamide

Cas No:200270-65-1

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