Structure and property based design of factor Xa inhibitors: Biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs

Autor:	Alan D. Borthwick, Marie Charbaut, Robert J. Young, Máire A. Convery, Ivan Leo Pinto, Andrew M. Mason, Weston Helen Elisabeth, Matthew Campbell, David W. Brown, Anthony J. Pateman, Henry Anderson Kelly, Derek Pollard, Shah Gita Punjabhai, John R. Toomey, N. Paul King, Stefan Senger, Eric Hortense, Ping Zhou, Hawa Diallo, Nigel S. Watson, Wendy R. Irving, Angela Patikis, Cynthia L. Burns-Kurtis, Savvas Kleanthous, Chuen Chan
Rok vydání:	2008
Předmět:	Male Models Molecular Serine Proteinase Inhibitors medicine.drug_mechanism_of_action Antithrombotic Agent Tertiary amine Stereochemistry Clinical Biochemistry Factor Xa Inhibitor Coagulation Factor Xa Pharmaceutical Science Biochemistry Chemical synthesis Rats Sprague-Dawley Structure-Activity Relationship Drug Discovery medicine Animals Molecular Biology chemistry.chemical_classification biology Chemistry Organic Chemistry Anticoagulants Stereoisomerism Bridged Bicyclo Compounds Heterocyclic Thiophene derivatives Pyrrolidinones Rats Sulfonamide Enzyme inhibitor biology.protein Molecular Medicine Hydrophobic and Hydrophilic Interactions Factor Xa Inhibitors
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 18:28-33
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2007.11.019
Popis:	Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating basic biaryl P4 groups, producing highly potent inhibitors with significant anticoagulant activities and encouraging oral pharmacokinetic profiles.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03145f782eb525e093f927857c7919cd https://doi.org/10.1016/j.bmcl.2007.11.019 Zobrazit plný text záznamu Full Text from ScienceDirect