Discovery of orally bioavailable NK1 receptor antagonists

Autor:	Bernard Christophe, T. Taverne, Patrick Pasau, Jean-Pierre Hénichart, Christophe Genicot, Florence Moureau, Luc Quere, Laurence Goossens, B. J. Van Keulen, Michel Gillard, Marie-Agnes Lassoie, Philippe Collart, Thomas Ryckmans, F. Stiernet, Jean-Marie Nicolas, Michel Neuwels
Rok vydání:	2003
Předmět:	Models Molecular Alkylation Chemical Phenomena Nitrogen Stereochemistry Acylation Carboxylic acid Guinea Pigs Clinical Biochemistry Carboxylic Acids Molecular Conformation Biological Availability Pharmaceutical Science Pulmonary Edema Ether CHO Cells Crystallography X-Ray Biochemistry Chemical synthesis Piperazines Structure-Activity Relationship chemistry.chemical_compound Neurokinin-1 Receptor Antagonists Oral administration Cricetinae Drug Discovery Animals Humans Structure–activity relationship Receptor Molecular Biology chemistry.chemical_classification Chemistry Physical Organic Chemistry Bioavailability chemistry Molecular Medicine Indicators and Reagents Selectivity
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 13:437-442
ISSN:	0960-894X
Popis:	Benzyloxyphenethylpiperazines are a new class of high affinity NK1 receptor antagonists. Oral bioavailability and selectivity can be fine tuned by the nature of the substituents on the basic nitrogen atom. Addition of substituents with a carboxylic acid group led to very selective and orally active NK1 antagonists free of interaction with L-type calcium channels.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::06f934cf18d1ae07e1b0903847f27e43 https://doi.org/10.1016/s0960-894x(02)00956-3 Zobrazit plný text záznamu Full Text from ScienceDirect