Imidazole derivatives of pyrrolidonic and piperidonic acids as potential inhibitors of human placental aromatase in vitro
| Autor: | Jacqueline Robert, Cuong Luu-Duc, Moomen Baroudi |
|---|---|
| Rok vydání: | 1996 |
| Předmět: |
Stereochemistry
Placenta Endocrinology Diabetes and Metabolism Clinical Biochemistry Drug Evaluation Preclinical Ring (chemistry) Biochemistry Structure-Activity Relationship chemistry.chemical_compound Endocrinology Non-competitive inhibition medicine Humans Imidazole Moiety Enzyme Inhibitors Aromatase Molecular Biology Piperidones chemistry.chemical_classification biology Aromatase Inhibitors Imidazoles Cell Biology Aminoglutethimide Pyrrolidinones Enzyme chemistry Enzyme inhibitor biology.protein Molecular Medicine medicine.drug |
| Zdroj: | The Journal of Steroid Biochemistry and Molecular Biology. 57:73-77 |
| ISSN: | 0960-0760 |
| DOI: | 10.1016/0960-0760(95)00253-7 |
| Popis: | Inhibitory activities towards human placental aromatase of novel pyrrolidinone and piperidinone drugs were investigated and compared with those of aminoglutethimide (AG) in vitro . All compounds showing a stronger inhibitory effect than this of AG had the following common structural feature: an imidazole side-chain in C-3 position, with a substituted or non-substituted aromatic ring in the C-2 position and an aliphatic chain ( n -butyl or n -octyl) or a phenyl moiety on the nitrogen of the pyrrolidone or piperidone ring. When the C-3 side-chain did not bear any imidazole ring, no activity was observed. Respective K i values for the competitive inhibition exerted by the more potent inhibitors 10, 11, 13 and 21 with androstenedione as substrate were 19.2, 20.3, 16.8 and 15.4 μM, respectively ( K i AG = 77.0 μM). |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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