Synthesis and in vitro evaluation of botryllazine B analogues as a new class of inhibitor against human aldose reductase

R Saito, M Tokita, K Uda, C Ishikawa, M Satoh

Index: Saito, Ryota; Tokita, Mai; Uda, Keisuke; Ishikawa, Chikako; Satoh, Mitsutoshi Tetrahedron, 2009 , vol. 65, # 15 p. 3019 - 3026

Full Text: HTML

Citation Number: 22

Abstract

Botryllazine B analogues of diverse substitution patterns have been prepared, and their in vitro inhibitory activities against recombinant human aldose reductase (h-ALR2) evaluated. Among the 15 compounds tested, 6-(4-aminophenyl)-2-(4-hydroxyphenyl) carbonylpyrazine (7b) proved to be the most potent inhibitor, with IC50= 0.91 μM. Kinetic analyses of 7b and botryllazine B (1) revealed that these inhibitors exhibit an unprecedented mixed-type ...