Synthesis and aldose reductase inhibitory activities of novel thienocinnolinone derivatives
Articolo
Data di Pubblicazione:
2004
Citazione:
Synthesis and aldose reductase inhibitory activities of novel thienocinnolinone derivatives / Pau, A., Asproni, B., Boatto, G., Grella, G.E., De Caprariis, P., Costantino, L., Pinna, G.A.. - In: EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES. - ISSN 0928-0987. - 21:4(2004), pp. 545-552. [10.1016/j.ejps.2003.12.005]
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.
© 2004 Elsevier B.V. All rights reserved.
Tipologia CRIS:
1.1 Articolo in rivista
Keywords:
Diabetic complications, Aldose reductase inhibitors, Thieno[h]cinnolinone carboxylic acids
Elenco autori:
Pau, Amedeo; Asproni, Battistina; Boatto, Gianpiero; Grella, Giuseppe Enrico; De Caprariis, P.; Costantino, L.; Pinna, Gerard Aime
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