Potent and selective bicyclic lactam inhibitors of thrombin: Part 3: P1′ modifications

Autor:	A. Susser, Peter D. Winocour, John DiMaio, Debra R. Holland, M. Arshad Siddiqui, Kent A. Berryman, Sophie Levesque, Janet S. Plummer, D. Lafleur, Jeremy J. Edmunds, Scott R. Eaton, J. Ronald Rubin, Annette Marian Doherty, Cuiman Cai, Wayne L. Cody, Stephen T. Rapundalo, Lakshmi S. Narasimhan, Yves St-Denis
Rok vydání:	1999
Předmět:	Models Molecular Lactams Stereochemistry Clinical Biochemistry Pharmaceutical Science Biochemistry Chemical synthesis Inhibitory Concentration 50 chemistry.chemical_compound Thrombin Heterocyclic Compounds Drug Discovery Antithrombotic medicine Animals Molecular Biology biology Bicyclic molecule Chemistry Organic Chemistry Active site Thrombosis Rats Disease Models Animal Kinetics Models Chemical Enzyme inhibitor biology.protein Lactam Molecular Medicine medicine.drug Discovery and development of direct thrombin inhibitors
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 9:835-840
ISSN:	0960-894X
DOI:	10.1016/s0960-894x(99)00096-7
Popis:	The synthesis and antithrombotic activity of a series of nonpeptide bicyclic thrombin inhibitors are described. We have explored the SAR around the P1' site. Modification of the P1' site has been found to affect potency and selectivity.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f3fd52bd5a522c0e984c8c93c262c0d https://doi.org/10.1016/s0960-894x(99)00096-7 Zobrazit plný text záznamu Full Text from ScienceDirect