1-(4-Amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine derivatives as melanin-concentrating hormone receptor-1 antagonists

Autor:	Mingzhu Zhang, David A. Schwarz, Tracy Baker, Val S. Goodfellow, Kathleen Gogas, Stacy Markison, Christopher E. Heise, Xiaochuan Wang, Yun-Fei Zhu, Charles Q. Huang, Takung Chen, Jun Fan
Rok vydání:	2005
Předmět:	Male Pyrrolidines Melanin-concentrating hormone Pyridines Stereochemistry Clinical Biochemistry Drug Evaluation Preclinical Administration Oral Biological Availability Pharmaceutical Science Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound In vivo Drug Discovery Animals Humans Structure–activity relationship Receptors Somatostatin Rats Wistar Molecular Biology Molecular Structure Body Weight Organic Chemistry In vitro Rats Melanin-concentrating hormone receptor Bioavailability chemistry Models Animal Molecular Medicine Amine gas treating
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 15:3701-3706
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2005.05.130
Popis:	Derivatives of 1-(4-amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine were identified as potent and functionally active MCH-R1 antagonists. One compound with Ki = 2.3 nM demonstrated good oral bioavailability (32%) and in vivo efficacy in rats.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1561713df671ea102232829150e9771 https://doi.org/10.1016/j.bmcl.2005.05.130 Zobrazit plný text záznamu Full Text from ScienceDirect