Novel xanthine oxidase inhibitor studies. Part 2. Synthesis and xanthine oxidase inhibitory activities of 2-substituted 6-alkylidenehydrazino- or 6-arylmethylidenehydrazino-7H-purines and 3- and/or 5-substituted 9H-1,2,4-triazolo[3,4-i[hair space]]purines

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Tomohisa Nagamatsu, Hiroo Yamasaki, Takayuki Fujita, Kazuki Endo and Haruhiko Machida


Abstract

The facile and general synthesis of 2-substituted 6-alkylidenehydrazino- or 6-arylmethylidenehydrazino-7H-purines and 3- and/or 5-substituted 9H-1,2,4-triazolo[3,4-i[hair space]]purines, which were obtained by oxidative cyclisation of the corresponding 6-aldehyde hydrazones of 7H-purine, as a new class of potential xanthine oxidase inhibitors are reported. Their inhibitory activities against bovine milk xanthine oxidase in vitro were also investigated, and some purines 2 and 6 and triazolopurines 7 exhibited from several times to several hundred times more potent activities than allopurinol.


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