Indoline and piperazine containing derivatives as a novel class of mixed D2/D4 receptor antagonists. Part 1: Identification and structure–activity relationships

Autor:	Hutchison Alan J, Kover Renata X, Robbin Brodbeck, Xiao-Shu He, Andrew Thurkauf, Kevin J. Hodgetts, Andrzej Kieltyka, Stanislaw Rachwal, Xiaoyan Zhang, John R. Peterson, Jan W. F. Wasley, Renee J. Primus, He Zhao
Rok vydání:	2002
Předmět:	Indoles medicine.drug_class Stereochemistry Clinical Biochemistry Glycine Pharmaceutical Science Carboxamide In Vitro Techniques Binding Competitive Biochemistry Chemical synthesis Piperazines Structure-Activity Relationship chemistry.chemical_compound Drug Discovery medicine Animals Humans Receptor Molecular Biology Bicyclic molecule Receptors Dopamine D4 Organic Chemistry Prazosin Recombinant Proteins Rats Dopamine D2 Receptor Antagonists Piperazine chemistry Indoline Dopamine Antagonists Molecular Medicine Lead compound
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 12:3105-3109
ISSN:	0960-894X
DOI:	10.1016/s0960-894x(02)00655-8
Popis:	Optimization of the lead compound 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2,3-dihydro-indol-1-yl)-ethanone 1 by systematic structure-activity relation (SAR) studies lead to two potent compounds 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2-methy-2,3-dihydro-indol-1-yl)-ethanone 2n and 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2-methy-2,3-dihydro-indol-1-yl)-ethanone 7b. Their related synthesis was also reported.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eb02ce198fbc302c0f8d14590d286292 https://doi.org/10.1016/s0960-894x(02)00655-8 Zobrazit plný text záznamu Full Text from ScienceDirect