Biagi G, Giorgi I, Livi O, Scartoni V, Tonetti I, Costantino L
Dipartimento di Scienze Farmaceutiche, Università di Pisa.
Farmaco. 1995 Apr;50(4):257-64.
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.
4(5)-氨基取代-5(4)-羧酰胺基-1H-1,2,3-三唑类化合物构成了一类新型的单环化合物，是有效的黄嘌呤氧化酶（XO）抑制剂。过去，这些化合物被错误地赋予了9-未取代-8-氮杂次黄嘌呤的结构。然而，本文描述了一些通过新的环化反应得到的8-氮杂次黄嘌呤。标题中的三唑类化合物的抑制活性高于相应的8-氮杂次黄嘌呤。4(5)-正戊氧基草酰氨基-5(4)-氨基甲酰基-1H-1,2,3-三唑对8-正戊基次黄嘌呤氧化的抑制竞争活性表明，该酶内仅存在一个亲脂性口袋。
