Synthesis and aldose reductase inhibitory activity of triazine derivatives possessing acetic acid group
Autor: | Pascal Coudert, Sylvie Mavel, P. Bastide, Catherine Rubat, P. Tronche, Jacques Couquelet, Eliane Albuisson, Eliane Duroux |
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Rok vydání: | 1992 |
Předmět: |
Tolrestat
Stereochemistry Carboxylic acid Acetates chemistry.chemical_compound Structure-Activity Relationship Aldehyde Reductase Drug Discovery medicine Structure–activity relationship Acetic Acid chemistry.chemical_classification Aldose reductase biology Triazines Biological activity General Chemistry General Medicine Aldose reductase inhibitor Enzyme chemistry Biochemistry Enzyme inhibitor biology.protein Pyrazoles medicine.drug |
Zdroj: | Chemicalpharmaceutical bulletin. 40(6) |
ISSN: | 0009-2363 |
Popis: | N-Acetic acid derivatives of 6-aryl-pyrazolo-triazin-4-ones were synthesized for evaluation as new aldose reductase inhibitors. The intrinsic activity of each compound was assessed by measuring the inhibition of enzymatic activity in an isolated pig lens enzyme preparation. All the prepared compounds exhibited a significant in vitro aldose reductase inhibitory effect (10(-6) M less than or equal to IC50 less than or equal to 10(-4) M). Furthermore, biological activity (log 1/IC50) for most of the data sets could be correlated directly to electronic and steric parameters. Finally, spatial configuration of the most active derivative 6c (IC50 = 2 x 10(-6) M) was compared with that of tolrestat and with pharmacophor requirements of the aldose reductase inhibitor site using a molecular modeling system. |
Databáze: | OpenAIRE |
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