Aminoquinazolines as TRPV1 antagonists: Modulation of drug-like properties through the exploration of 2-position substitution

Autor:	Rajagopal Bakthavatchalam, Lawrence K. Fung, Bertrand L. Chenard, David J. Matson, Chu K. Ngo, Marci Crandall, Stéphane De Lombaert, Daniel N. Cortright, Harry Brielmann, Charles A. Blum, Mark T. Kershaw, Jayaraman Chandrasekhar, Marta Day, Xiaozhang Zheng, James E. Krause, Kevin J. Hodgetts
Rok vydání:	2008
Předmět:	Drug ERG1 Potassium Channel Stereochemistry Chemistry Pharmaceutical media_common.quotation_subject Clinical Biochemistry Analgesic Molecular Conformation TRPV1 Pain TRPV Cation Channels Pharmaceutical Science Pharmacology Biochemistry Dogs Oral administration In vivo Drug Discovery medicine Animals Potency Molecular Biology media_common Inflammation Chemistry Organic Chemistry Antagonist Ether-A-Go-Go Potassium Channels Rats Kinetics Models Chemical Pharmaceutical Preparations Drug Design Hyperalgesia Aminoquinolines Molecular Medicine medicine.symptom
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 18:4573-4577
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2008.07.036
Popis:	A focused SAR exploration of the lead 4-aminoquinazoline TRPV1 antagonist 2 led to the discovery of compound 18. In rats, compound 18 is readily absorbed following oral dosing and demonstrates excellent in vivo potency and efficacy in an acute inflammatory pain model.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b27714146b399be27941a08e67faa5fd https://doi.org/10.1016/j.bmcl.2008.07.036 Zobrazit plný text záznamu Full Text from ScienceDirect