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 IC50 of 7.6 and 18 muM, 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.
Synthesis and aldose reductase inhibitory activities of novel thienocinnolinone derivatives / A., Pau; B., Asproni; G., Boatto; Ge, Grella; P., De Caprariis; Costantino, Luca; Ga, Pinna. - In: EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES. - ISSN 0928-0987. - STAMPA. - 21:(2004), pp. 545-552. [10.1016/j.ejps.2003.12.005]
Synthesis and aldose reductase inhibitory activities of novel thienocinnolinone derivatives
COSTANTINO, Luca;
2004
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 IC50 of 7.6 and 18 muM, 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.
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