New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems

Autor:	Paolo Celestini, Dieter Hamprecht, Romano Di Fabio, Anna Maria Capelli, Marcella Petrone, Giovanna Tedesco, Federica Damiani, Daniele Donati, Angela Worby, Silvia Terreni, Simone Braggio, Fabrizio Micheli, Stefania Gagliardi, Giorgio Bonanomi, Christian Heidbreder, Gabriella Gentile, Stefano Radaelli
Rok vydání:	2008
Předmět:	Molecular model Stereochemistry Clinical Biochemistry Pharmaceutical Science Biochemistry Chemical synthesis Benzazepine Structure-Activity Relationship chemistry.chemical_compound Dopamine receptor D3 Drug Discovery Animals Combinatorial Chemistry Techniques Moiety Molecular Biology chemistry.chemical_classification Molecular Structure Organic Chemistry Receptors Dopamine D3 Antagonist Benzazepines In vitro Rats chemistry Drug Design Dopamine Antagonists Molecular Medicine Tricyclic
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 18:901-907
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2007.12.066
Popis:	The synthesis and SAR of a new series of potent and selective dopamine D3 receptor antagonists is reported. The introduction of a tricyclic [h]-fused benzazepine moiety on the recently disclosed scaffold of 1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines is reported. A full rat pharmacokinetic characterization is also reported.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a6be4c784040906a4df98288c47711e https://doi.org/10.1016/j.bmcl.2007.12.066 Zobrazit plný text záznamu Full Text from ScienceDirect