Potent bicyclic lactam inhibitors of thrombin: Part I: P3 modifications

DOI: 10.1016/S0960-894X(98)00550-2

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 3193 - 3198 (1998)

Update date:2022-07-30

Topics:

Authors:

St-Denis, Yves

Augelli-Szafran, Corinne E.

Bachand, Benoit

Berryman, Kent A.

DiMaio, John

Doherty, Annette M.

Edmunds, Jeremy J.

Leblond, Lorraine

Levesque, Sophie

Narasimhan, Lakshmi S.

Penvose-Yi, Jan R.

Rubin, J. Ronald

Tarazi, Micheline

Winocour, Peter D.

Siddiqui, M. Arshad

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Article abstract of DOI:10.1016/S0960-894X(98)00550-2

Peptidomimetic inhibitors of general structure 1 have been prepared. Optimization of the binding affinities of these compounds through variation of the P3 hydrophobic residue is described. Selected substituted bicylic lactams displayed interesting pharmacological profiles both in vitro and in vivo.

Full text of DOI:10.1016/S0960-894X(98)00550-2

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