Coudert P, Duroux E, Bastide P, Couquelet J, Tronche P
Laboratoire de Chimie Thérapeutique, Faculté de Pharmacie, Clermond-Ferrand, France.
J Pharm Belg. 1991 Nov-Dec;46(6):375-80.
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.
已能够从4,6 - 二芳基哒嗪酮制备一系列在2 - 位被带有羧酸官能团的不同长度链取代的衍生物。对所有化合物评估了猪晶状体醛糖还原酶抑制活性。哒嗪环6 - 位苯核上带有氯原子的N - 乙酸衍生物3c是活性最高的哒嗪酮，IC50值为1.2×10⁻⁵ M。此外，已表明合成化合物的亲脂性和空间构型对酶活性起重要作用。
