Xanthine oxidase (XO). 4(5)-aminosubstituted-5(4)-carboxyamido-1H-1,2, 3-triazoles: a new class of monocyclic triazole inhibitors.
The 4(5)-aminosubstituted-5(4)-carboxyamido-1H-1,2,3-triazoles constitute a new class of monocyclic compounds as effective inhibitors of XO. In the past to these compounds the structure of 9-unsubstituted-8-azahypoxanthines was wrongly attributed. However some 8-azahypoxanthines obtained via a new annulation reaction have been described in this paper. The inhibitory activity of the title triazoles resulted greater than that shown by the corresponding 8-azahypoxanthines. The inhibitory competitive activity of 4(5)-n-pentyloxyoxalylamino-5(4)-carbamoyl-1H-1,2,3-triazole toward the oxidation of 8-n-pentylhypoxanthine disclosed that only one lipophilic pocket is present within the enzyme.
Biagi
G
G
Dipartimento di Scienze Farmaceutiche, Università di Pisa.
Giorgi
I
I
Livi
O
O
Scartoni
V
V
Tonetti
I
I
Costantino
L
L
D015394:Molecular Structure; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology*; D014969:Xanthine Oxidase / Q000037:antagonists & inhibitors*
D014230:Triazoles; D014969:Xanthine Oxidase