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

Autor:	Sophie Levesque, Kent A. Berryman, M. Arshad Siddiqui, Jeremy J. Edmunds, Peter D. Winocour, John DiMaio, Annette Marian Doherty, Yves St-Denis, C.E. Augelli-Szafran, Benoit Bachand, Lorraine Leblond, Lakshmi S. Narasimhan, J. Ronald Rubin, Micheline Tarazi, J.R. Penvose-Yi
Rok vydání:	1998
Předmět:	Serine Proteinase Inhibitors Lactams Molecular model medicine.drug_class Stereochemistry Peptidomimetic Clinical Biochemistry Pharmaceutical Science Carboxamide Crystallography X-Ray Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Thrombin Fibrinolytic Agents Drug Discovery medicine Animals Molecular Biology Bicyclic molecule biology Chemistry Organic Chemistry Rats Enzyme inhibitor Lactam biology.protein Molecular Medicine medicine.drug
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 8:3193-3198
ISSN:	0960-894X
DOI:	10.1016/s0960-894x(98)00550-2
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::197b252f0565e168178e927f9b2d1654 https://doi.org/10.1016/s0960-894x(98)00550-2 Zobrazit plný text záznamu Full Text from ScienceDirect