Potent P2Y1 urea antagonists bearing various cyclic amine scaffolds

Autor:	Qimin Wu, Alexandre L'Heureux, Christine Huang, Ji Hua, Robert P. Rehfuss, Jennifer X. Qiao, Laura Price, Patrick Y.S. Lam, Ming Chang, Ruth R. Wexler, Philippe Lapointe, Rejean Ruel, Alain Martel, Joanna Zheng, Carl Thibeault
Rok vydání:	2013
Předmět:	Blood Platelets Clinical Biochemistry Pharmaceutical Science Biochemistry P2y1 receptor chemistry.chemical_compound Receptors Purinergic P2Y1 Structure-Activity Relationship Piperidines Drug Discovery Aqueous solubility Organic chemistry Animals Humans Urea Amines Molecular Biology Organic Chemistry Purinergic receptor Isoindoline In vitro binding Rats Adenosine Diphosphate chemistry Microsomes Liver Molecular Medicine Amine gas treating Piperidine Purinergic P2Y Receptor Agonists Platelet Aggregation Inhibitors Half-Life Protein Binding
Zdroj:	Bioorganicmedicinal chemistry letters. 23(24)
ISSN:	1464-3405
Popis:	A number of new amine scaffolds with good inhibitory activity in the ADP-induced platelet aggregation assay have been found to be potent antagonists of the P2Y1 receptor. SAR optimization led to the identification of isoindoline 3c and piperidine 4a which showed good in vitro binding and functional activities, as well as improved aqueous solubility. Among them, the piperidine 4a showed the best overall profile with favorable PK parameters.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ce63ce6c7d5ef7678a2b3335fed8e2f6 https://pubmed.ncbi.nlm.nih.gov/24269480 Zobrazit plný text záznamu Full Text from ScienceDirect