Pau, Amedeo and Asproni, Battistina and Boatto, Gianpiero and Grella, Giuseppe Enrico and De Caprariis, Paolo and Costantino, Luca and Pinna, Gérard Aimé (2004) Synthesis and aldose reductase inhibitory activities of novel thienocinnolinone derivatives. European Journal of Pharmaceutical Sciences, Vol. 21 (4), p. 545-552. ISSN 0928-0987. Article.
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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 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.
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