Discovery libraries targeting the major enzyme classes: the serine hydrolases
| Autor: | Dale L. Boger, Venkat Srinivasan, Katerina Otrubova |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2014 |
| Předmět: |
Serine Proteinase Inhibitors
Stereochemistry Clinical Biochemistry Pharmaceutical Science Pyrazole Biochemistry Article Serine Small Molecule Libraries chemistry.chemical_compound Structure-Activity Relationship Fatty acid amide hydrolase Drug Discovery Structure–activity relationship Humans Molecular Biology Dose-Response Relationship Drug Molecular Structure Chemistry Drug discovery Organic Chemistry Serine hydrolase Molecular Medicine Serine Proteases HeLa Cells |
| Popis: | Two libraries of modestly reactive ureas containing either electron-deficient acyl anilines or acyl pyrazoles were prepared and are reported as screening libraries for candidate serine hydrolase inhibitors. Within each library is a small but powerful subset of compounds that serve as a chemotype fragment screening library capable of subsequent diversification. Elaboration of the pyrazole-based ureas provided remarkably potent irreversible structural inhibitors of fatty acid amide hydrolase (FAAH, apparent Ki = 100-200 pM) complementary to those previously disclosed enlisting electron-deficient aniline-based ureas. |
| Databáze: | OpenAIRE |
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