Synthesis and aldose reductase inhibitory activities of novel thienocinnolinone derivatives

Abstract A novel series of tetrahydrothieno[2,3- h ]cinnolinone derivatives were synthesized and evaluated in vitro for their ability to inhibit aldose reductase (ALR2), an enzyme involved in the appearance of diabetic complications. Compounds 2e and 2j exert a remarkable inhibitory effect, with IC 50 of 7.6 and 18 μM, respectively. These compounds incorporate a valid pharmacophore for aldose reductase inhibitory activity represented by a thienocinnolinone template linked through a pentamethylene spacer to a carboxylic function.