Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitors

DOI: 10.1016/S0960-894X(99)00483-7

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 2837 - 2842 (1999)

Update date:2022-08-05

Topics:

Authors:

Rewinkel

Lucas Lucas

Smit Smit

Noach Noach

Van Dinther

Rood Rood

Jenneboer

Van Boeckel

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Article abstract of DOI:10.1016/S0960-894X(99)00483-7

Replacement of the highly basic benzamidine moiety with moderate basic amino-bicycloaryl moieties in a series of thrombin inhibitors related to NAPAMP provided potent enzyme inhibition and significant improvements in membrane transport and oral bioavailability.

Full text of DOI:10.1016/S0960-894X(99)00483-7

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