Novel thioamide derivatives as neutral CB1 receptor antagonists
| Autor: | Erik Ryberg, Leifeng Cheng, Henrik Nordberg, Jonas Boström, Roine I. Olsson, Peter J. Greasley, Joakim Tholander, Stephan Hjorth |
|---|---|
| Rok vydání: | 2009 |
| Předmět: |
Stereochemistry
medicine.drug_class Clinical Biochemistry Pharmaceutical Science Mice Obese Carboxamide Biochemistry Chemical synthesis chemistry.chemical_compound Mice Structure-Activity Relationship Receptor Cannabinoid CB1 Drug Discovery medicine Animals Obesity Receptor Molecular Biology Thioamide chemistry.chemical_classification Organic Chemistry Antagonist Biological activity Thioamides Disease Models Animal chemistry Pyrazines Molecular Medicine Lawesson's reagent Anti-Obesity Agents Linker |
| Zdroj: | Bioorganicmedicinal chemistry letters. 20(2) |
| ISSN: | 1464-3405 |
| Popis: | A novel class of cannabinoid-1 (CB1) receptor antagonists for the treatment of obesity is presented. The carboxamide linker in a set of 5,6-diaryl-pyrazine-2-amide derivatives was transformed into the corresponding thioamide, by using a one-pot synthesis. The structural series of thioamides not only showed retained CB1 potency (below 10 nM), but also showed improved solubility. In addition, the neutral antagonist 2c significantly reduced body weight in cafeteria diet obese mice. |
| Databáze: | OpenAIRE |
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