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Thienocinnolinone alkanoic acid derivatives as aldose reductase inhibitors

Pau, Amedeo and Asproni, Battistina and Murineddu, Gabriele and Boatto, Gianpiero and Grella, Giuseppe Enrico and Rakowitz, Dietmar and Costantino, Luca and Pinna, Gérard Aimé (2006) Thienocinnolinone alkanoic acid derivatives as aldose reductase inhibitors. Medicinal Chemistry, Vol. 2 (1), 39-45(7). ISSN 1573-4064. Article.

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A new series of 8-halogen-4,4a,5,6-tetrahydrothieno[2,3-h]cinnolinone-N2-alkanoic acids was prepared and tested for aldose reductase (ALR2) inhibitory activities. These compounds showed significant inhibitory activity against bovine lens ALR2, with the best compound 2e showing an IC50 value of 31.4 μM. The presence of the C8-substituents here studied (Cl, Br) on the thienocinnolinone scaffold caused a decrease of the inhibitory potency by a factor of about 4 with respect to the unsubstituted parent compound, while the presence of a C8-methyl group, considered in a previous paper [1] decreased the activity by a factor of about 2. Moreover, the length of the N2 alkanoic chain influences strongly the enzyme inhibitory activity. While most of the carboxylic acids ALR2 inhibitors are acetic acid derivatives, in the case of thienocinnolinone compounds, homologues higher than acetic acids showed to be more active.

Item Type:Article
ID Code:4427
Uncontrolled Keywords:Aldose reductase inhibitors, carboxylic acids, diabetic complications, thieno[h]cinnolinone
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:Bentham Science
Deposited On:31 Aug 2010 18:34

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