1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors

DOI: 10.1016/S0960-894X(99)00069-4

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 685 - 690 (1999)

Update date:2022-07-29

Topics:

Authors:

Rewinkel

Lucas Lucas

Van Galen

Noach Noach

Van Dinther

Rood Rood

Jenneboer

Van Boeckel

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Article abstract of DOI:10.1016/S0960-894X(99)00069-4

Replacement of the highly basic benzamidine moiety of NAPAP by the moderately basic 1-aminoisoquinoline moiety resulted in thrombin inhibitors with improved selectivity towards trypsin and enhanced Caco-2 cell permeability.

Full text of DOI:10.1016/S0960-894X(99)00069-4

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