Synthesis and Biochemical Testing of 3-(Carboxyphenylethyl)imidazo[2,1-f][1,2,4]triazines as Inhibitors of AMP Deaminase
作者： Stephen D. Lindell , Simon Maechling , Richard L. Sabina
DOI: 10.1021/ML100092A
关键词: Triazine 、 Stereochemistry 、 AMP deaminase 、 Biology 、 Isozyme 、 Recombinant DNA 、 Ribose phosphate 、 IC50 、 Aglycone 、 Biochemical testing
摘要: C-Ribosyl imidazo[2,1-f][1,2,4]triazines and 3-[2-(3-carboxyphenyl)ethyl]-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ols represent two classes of known AMP deaminase inhibitors. A combination the aglycone from former class with ribose phosphate mimic latter led to 3-[2-(3-carboxyphenyl)ethyl]imidazo[2,1-f][1,2,4]triazines, which a new The best compound, 3-[2-(3-carboxy-5,6,7,8-tetrahydronaphthyl)ethyl]imidazo[2,1-f][1,2,4]triazine (8), was good inhibitor all three human AMPD recombinant isozymes (AMPD1, AMPD2, AMPD3; IC50 = 0.9−5.7 μM) but poor plant enzyme (Arabidopsis FAC1; 200 μM).
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