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2010 ; 1
(6
): 286-9
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English Wikipedia
Synthesis and Biochemical Testing of
3-(Carboxyphenylethyl)imidazo 2,1-f 1,2,4 triazines as Inhibitors of AMP
Deaminase
#MMPMID24900209
Lindell SD
; Maechling S
; Sabina RL
ACS Med Chem Lett
2010[Sep]; 1
(6
): 286-9
PMID24900209
show ga
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 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-f][1,2,4]triazine
(8), was a good inhibitor of all three human AMPD recombinant isozymes (AMPD1,
AMPD2, and AMPD3; IC50 = 0.9-5.7 ?M) but a poor inhibitor of the plant
recombinant enzyme (Arabidopsis FAC1; IC50 = 200 ?M).