[Synthesis and evaluation of the aldose reductase inhibitory activity of new diaryl pyridazine-3-ones]

Autor: P, Coudert, E, Duroux, P, Bastide, J, Couquelet, P, Tronche
Jazyk: francouzština
Rok vydání: 1991
Předmět:
Zdroj: Journal de pharmacie de Belgique. 46(6)
ISSN: 0047-2166
Popis: It has been possible to prepare from 4,6-diaryl pyridazinones a series of derivatives substituted in the 2-position by chains of various lengths bearing a carboxylic acid function. Pig lens aldose reductase inhibitory activity was evaluated for all compounds. N-acetic acid derivative 3c with a chlorine atom on the phenyl nucleus at the 6-position on the pyridazin ring was the most active pyridazinone with an IC50 value of 1.2 x 10(-5) M. Furthermore, it has been shown that lipophilicity and spatial configuration of the synthesized compounds took a prominent part on enzymatic activity.
Databáze: OpenAIRE