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[摘要]：C-Ribosyl imidazo[2,1-f][1,2,4]triazines and 3-[2-(3-carboxypheny1)ethyl]-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diaze pin-8-ols represent two classes of known AMP deaminase inhibitors. A combination of the aglycone from the former class with the ribose phosphate mimic from the latter led to the 3-[2-(3-carboxyphenyl)ethyl]imidazo[2, 1-f][1,2,4]triazines, which represent a new class of AMP deaminase inhibitors. The best compound, 3-[2-(3-carboxy-5.6,7,8-tetrahydronaphthyl)ethyl]imidazo[2,1,2,4]triazi ne (8), was a good inhibitor of all three human AMPD recombinant isozymes (AMPD1, AMPD2, and AMPD3;IC50 = 0.9-5.7 mu M) but a poor inhibitor of the plant recombinant enzyme (Arabidopsis FAC1; IC50 = 200 mu M). |
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