Document Detail


Identification of 2-aminobenzimidazoles as potent melanin-concentrating hormone 1-receptor (MCH1R) antagonists.
MedLine Citation:
PMID:  19457661     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A series of 2-aminobenzimidazole-based MCH1R antagonists was identified by core replacement of the aminoquinoline lead 1. Subsequent modification of the 2- and 5-positions led to improvement in potency and intrinsic clearance. Compound 25 exhibited good plasma and brain exposure, and attenuated MCH induced food intake at 30mg/kg PO in rats.
Authors:
Minoru Moriya; Hiroyuki Kishino; Shunji Sakuraba; Toshihiro Sakamoto; Takuya Suga; Hidekazu Takahashi; Takao Suzuki; Masahiko Ito; Junko Ito; Ryuichi Moriya; Norihiro Takenaga; Hisashi Iwaasa; Akane Ishihara; Akio Kanatani; Takehiro Fukami
Publication Detail:
Type:  Journal Article     Date:  2009-05-05
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  19     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2009 Jul 
Date Detail:
Created Date:  2009-06-09     Completed Date:  2009-09-01     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  3568-72     Citation Subset:  IM    
Affiliation:
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd, Okubo-3, Tsukuba, Ibaraki 300-2611, Japan. minoru_moriya@merck.com
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MeSH Terms
Descriptor/Qualifier:
Animals
Anti-Obesity Agents / chemical synthesis,  chemistry*,  pharmacokinetics
Benzimidazoles / chemical synthesis,  chemistry*,  pharmacokinetics
Eating / drug effects
Rats
Rats, Sprague-Dawley
Receptors, Somatostatin / antagonists & inhibitors*,  metabolism
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/Anti-Obesity Agents; 0/Benzimidazoles; 0/Mch1r protein, rat; 0/Receptors, Somatostatin; 934-32-7/2-aminobenzimidazole

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