Abstract
For investigation of the structure-activity relationship of xanthine derivatives, 2, 4-dioxo-1, 2, 3, 4-tetrahydropyrrolo [2, 3-d] pyrimidines (A), which belong to 7-deazaxanthine derivatives, were prepared from the corresponding 6-aminouracils and chloroacetaldehyde, and then were catalytically reduced to give 2, 4-dioxo-1, 2, 3, 4, 5, 6-hexahydropyrrolo [2, 3-d]-pyrimidines (B). A new method for synthesis of compounds (A) was found by heating 6-hydrazinouracil derivatives with aldehydes or ketones. Diuretic, cardiac, and central nervous system stimulating activities of compounds (A and B) were tested to be compared with those of caffeine. Compounds (A and B) showed caffeine-like activities.
