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]
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Titolo: | Synthesis and aldose reductase inhibitory activities of novel thienocinnolinone derivatives | |
Autori: | ||
Data di pubblicazione: | 2004 | |
Rivista: | ||
Citazione: | 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] | |
Handle: | http://hdl.handle.net/11388/61248 | |
Appare nelle tipologie: | 1.1 Articolo in rivista |