An orally active corticotropin releasing factor 1 receptor antagonist from 8-aryl-1,3a,7,8-tetraaza-cyclopenta[a]indenes

Autor:	Tracey Fiedler, Matthew T. Taber, Jie Zhang, Shelly X. Ren, Robert Macci, Sokhom S. Pin, Gene M. Dubowchik, Kaitlin E. Browman, Lynn A. Balanda, Jay O. Knipe, Kevin D. Burris, Rita L. Civiello, Xiaojun Han
Rok vydání:	2007
Předmět:	Time Factors Tertiary amine medicine.drug_class Stereochemistry Clinical Biochemistry Administration Oral Pharmaceutical Science Receptors Corticotropin-Releasing Hormone Biochemistry Anxiolytic Chemical synthesis Mice Structure-Activity Relationship chemistry.chemical_compound Drug Discovery medicine Animals Receptor Molecular Biology chemistry.chemical_classification Aza Compounds Mice Inbred BALB C Dose-Response Relationship Drug Depression Aryl Organic Chemistry Antagonist Water Receptor antagonist Antidepressive Agents Kinetics Indenes Models Chemical Solubility chemistry Molecular Medicine Tricyclic
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 17:2026-2030
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2007.01.008
Popis:	8-Aryl-1,3a,7,8-tetraaza-cyclopenta[a]indenes represent a novel series of high-affinity corticotropin-releasing factor-1 receptor (CRF1R) antagonists. Herein we report the synthesis and SAR around the tricyclic core and the anxiolytic activity of an orally dosed exemplary compound 9d (Ki = 8.0 nM) in a mouse canopy model.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af1143383cd229586f3c2af1512e57b5 https://doi.org/10.1016/j.bmcl.2007.01.008 Zobrazit plný text záznamu Full Text from ScienceDirect