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 M, 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. © 2004 Elsevier B.V. All rights reserved.
Synthesis and aldose reductase inhibitory activities of novel thienocinnolinone derivatives / Pau, Amedeo; Asproni, Battistina; Boatto, Gianpiero; Grella, Giuseppe Enrico; De Caprariis, P.; Costantino, L.; Pinna, Gerard Aime. - In: EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES. - ISSN 0928-0987. - 21:4(2004), pp. 545-552. [10.1016/j.ejps.2003.12.005]
Synthesis and aldose reductase inhibitory activities of novel thienocinnolinone derivatives
ASPRONI, Battistina;BOATTO, Gianpiero;PINNA, Gerard Aime
2004-01-01
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 M, 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. © 2004 Elsevier B.V. All rights reserved.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
