Document Detail

Discovery of novel spiro-piperidine derivatives as highly potent and selective melanin-concentrating hormone 1 receptor antagonists.
MedLine Citation:
PMID:  19403308     Owner:  NLM     Status:  MEDLINE    
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 IC(50) value of 0.09 nM at hMCH-1R. The synthesis and structure-activity relationships of the novel spiro-piperidine MCH-1R antagonists are described.
Takao Suzuki; Minoru Moriya; Toshihiro Sakamoto; Takuya Suga; Hiroyuki Kishino; Hidekazu Takahashi; Makoto Ishikawa; Keita Nagai; Yumiko Imai; Etsuko Sekino; Masahiko Ito; Hisashi Iwaasa; Akane Ishihara; Shigeru Tokita; Akio Kanatani; Nagaaki Sato; Takehiro Fukami
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Publication Detail:
Type:  Journal Article     Date:  2009-04-09
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  19     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2009 Jun 
Date Detail:
Created Date:  2009-05-15     Completed Date:  2009-07-17     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  3072-7     Citation Subset:  IM    
Department of Medicinal Chemistry, Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co, Ltd, Tsukuba, Ibaraki, Japan.
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MeSH Terms
Cell Line
Drug Discovery
Piperidines / chemical synthesis,  chemistry*,  pharmacology
Receptors, Somatostatin / antagonists & inhibitors*,  metabolism
Spiro Compounds / chemical synthesis,  chemistry*,  pharmacology
Structure-Activity Relationship
Reg. No./Substance:
0/MCHR1 protein, human; 0/Piperidines; 0/Receptors, Somatostatin; 0/Spiro Compounds

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