Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1

Autor:	Stephen J. Medhurst, Sandra Arpino, James Wright, Darren Jason Mitchell, Alexander J. Stevens, James Biggs, Kim Winborn, Susan Marie Westaway, John B. Davis, Jeffrey C. Jerman, Vicky Holland, Tanya Coleman, Jennifer E. Cryan, Geoffrey Stemp, Sarah C. Lappin, Jon T. Seal, Harshad Kantilal Rami, Leontine Saskia Trouw, Mervyn Thompson, Martin J. Gunthorpe
Rok vydání:	2008
Předmět:	Niacinamide Stereochemistry medicine.drug_class Chemistry Pharmaceutical Clinical Biochemistry Analgesic Guinea Pigs TRPV1 Pharmaceutical Science Administration Oral TRPV Cation Channels Carboxamide Biochemistry Chemical synthesis Cell Line chemistry.chemical_compound Inhibitory Concentration 50 In vivo Drug Discovery medicine Animals Humans Benzothiazoles Molecular Biology Inflammation Nicotinamide Chemistry Organic Chemistry Antagonist In vitro Rats Models Chemical Drug Design Molecular Medicine Capsaicin
Zdroj:	Bioorganicmedicinal chemistry letters. 18(20)
ISSN:	1464-3405
Popis:	6-Phenylnicotinamide (2) was previously identified as a potent TRPV1 antagonist with activity in an in vivo model of inflammatory pain. Optimization of this lead through modification of both the biaryl and heteroaryl components has resulted in the discovery of 6-(4-fluorophenyl)-2-methyl-N-(2-methylbenzothiazol-5-yl)nicotinamide (32; SB-782443) which possesses an excellent overall profile and has been progressed into pre-clinical development.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87b365ea545812a5b73fbe175229b22f https://pubmed.ncbi.nlm.nih.gov/18809327 Zobrazit plný text záznamu Full Text from ScienceDirect