Following our previous studies on pyridazinone carboxylic acids as potent and selective aldose reductase (ALR2) inhibitors, a new series of benzo[h]cinnolinone carboxylic acids, variously substituted at the positions 4, 7-10 and differently modified both at the central ring and at the acidic side chain, were synthesized and tested as inhibitors of ALR2. Comparison with previously synthesized compounds allows us to define more precisely structure-activity relationships for this class of compounds. In fact, in addition to the importance of the acidic side chain, their properties are highly influenced by the substituents present on the benzo[h]cinnolinone nucleous, with potency ranging from that of Sorbinil to very weakly active compounds.

Synthesis and aldose reductase inhibitory activity of a new series of benzo[h]cinnolinone derivatives / Costantino, Luca; Rastelli, Giulio; G., Cignarella; D., Barlocco. - In: IL FARMACO. - ISSN 0014-827X. - STAMPA. - 55(2000), pp. 544-552. [10.1016/S0014-827X(00)00035-5]

Synthesis and aldose reductase inhibitory activity of a new series of benzo[h]cinnolinone derivatives

COSTANTINO, Luca;RASTELLI, Giulio;
2000

Abstract

Following our previous studies on pyridazinone carboxylic acids as potent and selective aldose reductase (ALR2) inhibitors, a new series of benzo[h]cinnolinone carboxylic acids, variously substituted at the positions 4, 7-10 and differently modified both at the central ring and at the acidic side chain, were synthesized and tested as inhibitors of ALR2. Comparison with previously synthesized compounds allows us to define more precisely structure-activity relationships for this class of compounds. In fact, in addition to the importance of the acidic side chain, their properties are highly influenced by the substituents present on the benzo[h]cinnolinone nucleous, with potency ranging from that of Sorbinil to very weakly active compounds.
55
544
552
Synthesis and aldose reductase inhibitory activity of a new series of benzo[h]cinnolinone derivatives / Costantino, Luca; Rastelli, Giulio; G., Cignarella; D., Barlocco. - In: IL FARMACO. - ISSN 0014-827X. - STAMPA. - 55(2000), pp. 544-552. [10.1016/S0014-827X(00)00035-5]
Costantino, Luca; Rastelli, Giulio; G., Cignarella; D., Barlocco
File in questo prodotto:
File Dimensione Formato  
Synthesis-and-ALR2-inhibitory-activity-cinnolinone-Farmaco2000.pdf

non disponibili

Tipologia: Versione dell'editore (versione pubblicata)
Dimensione 132.69 kB
Formato Adobe PDF
132.69 kB Adobe PDF   Visualizza/Apri   Richiedi una copia
Pubblicazioni consigliate

Caricamento pubblicazioni consigliate

Licenza Creative Commons
I metadati presenti in IRIS UNIMORE sono rilasciati con licenza Creative Commons CC0 1.0 Universal, mentre i file delle pubblicazioni sono rilasciati con licenza Attribuzione 4.0 Internazionale (CC BY 4.0), salvo diversa indicazione.
In caso di violazione di copyright, contattare Supporto Iris

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11380/458216
Citazioni
  • ???jsp.display-item.citation.pmc??? 0
  • Scopus 23
  • ???jsp.display-item.citation.isi??? 21
social impact