Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists

Autor:	Etsuko Sekino, Akio Kanatani, Hisashi Iwaasa, Masahiko Ito, Minoru Moriya, Akane Ishihara, Junko Ito, Yuji Haga, Norikazu Ohtake, Makoto Ando
Rok vydání:	2009
Předmět:	Melanin-concentrating hormone Stereochemistry Pyridones Clinical Biochemistry Pharmaceutical Science CHO Cells Biochemistry Chemical synthesis chemistry.chemical_compound Mice Structure-Activity Relationship Cricetulus Cricetinae Drug Discovery Moiety Structure–activity relationship Animals Humans Receptors Somatostatin Receptor Molecular Biology Chemistry Drug discovery Chinese hamster ovary cell Organic Chemistry Recombinant Proteins Lactam Microsomes Liver Molecular Medicine Anti-Obesity Agents
Zdroj:	Bioorganicmedicinal chemistry letters. 19(17)
ISSN:	1464-3405
Popis:	Novel phenethylpyridone derivatives were identified as potent human melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. A search for surrogates for the 4-(2-aminoethoxy)phenyl moiety of 1 resulted in discovery of 2-[4-(aminomethyl)phenyl]ethyl substructure as in 6a. Successive optimization of the right-hand moiety led to the identification of a number of potent derivatives.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f1f099231e52a67ac8afa97c6a90ccb https://pubmed.ncbi.nlm.nih.gov/19632840 Zobrazit plný text záznamu Full Text from ScienceDirect