5,6-Diphenylpyridazine Derivatives as Acyl-CoA:Cholesterol Acyltransferase Inhibitors
| Autor: | L. Toma, Maria Palola Giovannoni, Monica Canavesi, Franco Bernini, Vittorio Dal Piaz, Young-Kook Kim, Daniela Barlocco, Byoung-Mog Kwon, Mi Kyung Kim |
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| Rok vydání: | 2001 |
| Předmět: |
Models
Molecular Stereochemistry Sterol O-acyltransferase In Vitro Techniques Chemical synthesis Mice Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Animals Enzyme Inhibitors chemistry.chemical_classification Cell-Free System biology Cholesterol Macrophages In vitro Rats Pyridazines Enzyme Biochemistry chemistry Enzyme inhibitor Acyltransferases Microsomes Liver Microsome biology.protein Molecular Medicine Sterol O-Acyltransferase |
| Zdroj: | Journal of Medicinal Chemistry. 44:4292-4295 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm010807h |
| Popis: | Alkyl-5,6-diphenylpyridazine derivatives combining several main features of ACAT inhibitors, such as a long alkyl side chain linked to a heterocycle and the o-diphenyl system, were synthesized and tested. Moreover, modeling studies on representative terms were performed. Some compounds displayed ACAT inhibition in the micromolar range, both on the enzyme isolated from rat liver microsomes and in cell-free homogenate of murine macrophages. |
| Databáze: | OpenAIRE |
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