| Discovery of imidazole carboxamides as potent and selective CCK1R agonists. | |
| | |
MedLine Citation:
|
PMID: 18614364 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
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. |
| | |
Authors:
|
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 |
Related Documents
:
|
2415364 - Kinetics of the inhibition of food-stimulated secretion by ranitidine in dogs. 20938444 - Meal size can be decreased in obese subjects through pharmacological acceleration of ga... 2360554 - Changes in eating behavior after horizontal gastroplasty and roux-en-y gastric bypass. 6143304 - Analysis of food stimulation of gastrin release in dogs by a panel of inhibitors. 16786244 - New solid-state fermentation chamber for bulk production of aerial conidia of fungal bi... 22117664 - Adverse food reactions-an emerging issue for adults. |
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 |
Affiliation:
|
Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA. cheng_zhu@merck.com |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Amides
/
chemical synthesis*,
chemistry,
pharmacology* Animals Anti-Obesity Agents / chemical synthesis*, chemistry, pharmacology* Combinatorial Chemistry Techniques Eating / drug effects Gallbladder Emptying / drug effects Humans Imidazoles / chemical synthesis*, chemistry, pharmacology* Mice Molecular Structure Receptors, Cholecystokinin / agonists* Structure-Activity Relationship |
| Chemical | |
Reg. No./Substance:
|
0/Amides; 0/Anti-Obesity Agents; 0/CCK1 protein, mouse; 0/Imidazoles; 0/Receptors, Cholecystokinin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Adsorptive removal of copper and nickel ions from water using chitosan coated PVC beads.
Next Document: Successful kinase bypass with new acyclovir phosphoramidate prodrugs.