Document Detail

Discovery of imidazole carboxamides as potent and selective CCK1R agonists.
MedLine Citation:
PMID:  18614364     Owner:  NLM     Status:  MEDLINE    
High-throughput screening revealed diaryl pyrazole 3 as a selective albeit modest cholecystokinin 1 receptor (CCK1R) agonist. SAR studies led to the discovery and optimization of a novel class of 1,2-diaryl imidazole carboxamides. Compound 44, which was profiled extensively, showed good in vivo mouse gallbladder emptying (mGBE) and lean mouse overnight food intake (ONFI) reduction activities.
Cheng Zhu; Alexa R Hansen; Thomas Bateman; Zhesheng Chen; Tom G Holt; James A Hubert; Bindhu V Karanam; Susan J Lee; Jie Pan; Su Qian; Vijay B G Reddy; Marc L Reitman; Alison M Strack; Vincent Tong; Drew T Weingarth; Michael S Wolff; Doug J MacNeil; Ann E Weber; Joseph L Duffy; Scott D Edmondson
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Publication Detail:
Type:  Journal Article     Date:  2008-06-20
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  18     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2008 Aug 
Date Detail:
Created Date:  2008-07-29     Completed Date:  2008-08-22     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  4393-6     Citation Subset:  IM    
Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA.
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MeSH Terms
Amides / chemical synthesis*,  chemistry,  pharmacology*
Anti-Obesity Agents / chemical synthesis*,  chemistry,  pharmacology*
Combinatorial Chemistry Techniques
Eating / drug effects
Gallbladder Emptying / drug effects
Imidazoles / chemical synthesis*,  chemistry,  pharmacology*
Molecular Structure
Receptors, Cholecystokinin / agonists*
Structure-Activity Relationship
Reg. No./Substance:
0/Amides; 0/Anti-Obesity Agents; 0/CCK1 protein, mouse; 0/Imidazoles; 0/Receptors, Cholecystokinin

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