Discovery of novel spiro-piperidine derivatives as highly potent and selective melanin-concentrating hormone 1 receptor antagonists

Autor:	Takehiro Fukami, Hisashi Iwaasa, Keita Nagai, Etsuko Sekino, Takuya Suga, Akio Kanatani, Toshihiro Sakamoto, Makoto Ishikawa, Nagaaki Sato, Masahiko Ito, Hidekazu Takahashi, Minoru Moriya, Yumiko Imai, Shigeru Tokita, Takao Suzuki, Akane Ishihara, Hiroyuki Kishino
Rok vydání:	2009
Předmět:	Melanin-concentrating hormone medicine.drug_class Stereochemistry Clinical Biochemistry Pharmaceutical Science Carboxamide Biochemistry Chemical synthesis Cell Line chemistry.chemical_compound Structure-Activity Relationship Piperidines Drug Discovery medicine Humans Spiro Compounds Receptors Somatostatin Receptor Molecular Biology IC50 Chemistry Organic Chemistry Antagonist respiratory system In vitro Molecular Medicine Piperidine hormones hormone substitutes and hormone antagonists
Zdroj:	Bioorganicmedicinal chemistry letters. 19(11)
ISSN:	1464-3405
Popis:	Optimization of high-throughput screening hit 1a led to the identification of a novel spiro-piperidine class of melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. Compound 3c was identified as a highly potent and selective MCH-1R antagonist, which has an IC50 value of 0.09 nM at hMCH-1R. The synthesis and structure–activity relationships of the novel spiro-piperidine MCH-1R antagonists are described.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99f0b40987aa1a2273688f6eee24d105 https://pubmed.ncbi.nlm.nih.gov/19403308 Zobrazit plný text záznamu Full Text from ScienceDirect