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Aminocyclitol and iminosugar derivatives related to Gauche disease

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Aminocyclitol and iminosugar derivatives

related to Gauche disease

Ester Monlleó Mas

Aquesta tesi doctoral està subjecta a la llicència Reconeixement 3.0. Espanya de Creative

Commons.

Esta tesis doctoral está sujeta a la licencia Reconocimiento 3.0. España de Creative

Commons.

(2)

log [ ] (M) % i m ig lu c e ra s e i n h ib it io n -12 -10 -8 -6 -4 0 50 100 pH 5.2 pH 7.0 Bottom Top LogIC50 IC50 Span pH 5.2 99.64 4.416 -7.102 7.902e-008 -95.22 pH 7.0 96.93 3.015 -7.348 4.485e-008 -93.92

(3)

log [ ] (M) % i m ig lu c e ra s e i n h ib it io n -12 -10 -8 -6 -4 -2 0 50 100 pH 5.2 pH 7.0 Bottom Top LogIC50 IC50 Span pH 5.2 98.95 4.552 -5.229 5.902e-006 -94.40 pH 7.0 99.85 3.064 -5.176 6.670e-006 -96.79

pH 5.2: three independent assays with triplicates pH 7.0: single assay with triplicates

(4)

log [ ] (M) % i m ig lu c e ra s e i n h ib it io n -12 -10 -8 -6 -4 -2 0 50 100 pH 5.2 pH 7.0 Best-fit values Bottom Top LogIC50 IC50 Span pH 5.2 97.22 -3.072 -4.563 2.738e-005 -100.3 pH 7.0 99.46 4.156 -5.140 7.241e-006 -95.30

(5)

log [ ] (M) -12 -10 -8 -6 -4 -2 0 50 100 pH 5.2 pH 7.0 Best-fit values Bottom Top LogIC50 IC50 Span pH 5.2 98.36 3.185 -6.954 1.112e-007 -95.17 pH 7.0 100.5 -1.315 -7.774 1.683e-008 -101.8

(6)

log [ ] (M) % i m ig lu c e ra s e i n h ib it io n -12 -10 -8 -6 -4 0 50 100 pH 5.2 pH 7.0 Bottom Top LogIC50 IC50 Span pH 5.2 100.2 2.216 -5.677 2.103e-006 -98.02 pH 7.0 97.57 4.591 -5.910 1.230e-006 -92.98

(7)

log [ ] (M) % i m ig lu c e ra s e i n h ib it io n -12 -10 -8 -6 -4 0 50 100 pH 7.0 pH 5.2 Bottom Top LogIC50 IC50 Span pH 5.2 99.77 2.270 -5.532 2.941e-006 -97.50 pH 7.0 98.08 2.105 -5.306 4.943e-006 -95.98

(8)

log [ ] (M) % i m ig lu c e ra s e i n h ib it io n -12 -10 -8 -6 -4 -2 0 50 100 pH 7.0 Best-fit values Bottom Top LogIC50 IC50 Span pH 5.2 100.1 -0.9038 -5.674 2.120e-006 -101.0 pH 7.0 100.2 -0.01262 -6.613 2.438e-007 -100.3 pH 5.2

(9)

log [ ] (M) % i m ig lu c e ra s e i n h ib it io n -9 -8 -7 -6 -5 -4 -3 -2 0 50 100 pH 5.2 pH 7.0 Best-fit values Bottom Top LogIC50 IC50 Span pH 5.2 97.45 2.967 -3.380 0.0004167 -94.49 pH 7.0 97.61 1.396 -3.911 0.0001228 -96.21

(10)

log [ ] (M) % i m ig lu c e ra s e i n h ib it io n -12 -10 -8 -6 -4 0 50 100 Bottom Top LogIC50 IC50 Span pH 5.2 99.98 3.809 -7.190 6.457e-008 -96.17 pH 7.0 101.1 -1.397 -8.127 7.461e-009 -102.5 pH 5.2 pH 7.0

(11)

log [ ] (M) % i m ig lu c e ra s e i n h ib it io n -10 -8 -6 -4 -2 0 50 100 Bottom Top LogIC50 IC50 Span pH 5.2 97.78 2.794 -4.152 7.053e-005 -94.99 pH 7.0 97.70 1.096 -4.916 1.212e-005 -96.60 pH 5.2 pH 7.0

(12)

log [ ] (M) % i m ig lu c e ra s e i n h ib it io n -12 -10 -8 -6 -4 0 50 100 pH 5.2 pH 7.0 Best-fit values Bottom Top LogIC50 IC50 Span pH 5.2 99.50 3.088 -6.621 2.393e-007 -96.41 pH 7.0 99.39 1.452 -7.621 2.394e-008 -97.94

(13)

log [ ] (M) % i m ig lu c e ra s e i n h ib it io n -12 -10 -8 -6 -4 0 50 100 pH 5.2 pH 7.0 Bottom Top LogIC50 IC50 Span pH 5.2 102.9 3.362 -5.338 4.589e-006 -99.53 pH 7.0 95.74 -2.143 -5.100 7.938e-006 -97.88

(14)

log [ ] (M) % i m ig lu c e ra s e i n h ib it io n -12 -10 -8 -6 -4 0 50 100 pH 5.2 pH 7.0 Best-fit values Bottom Top LogIC50 IC50 Span pH 5.2 101.9 -0.1443 -6.032 9.293e-007 -102.1 pH 7.0 100.9 0.2595 -6.596 2.536e-007 -100.6

(15)

log [ ] (M) % i m ig lu c e ra s e i n h ib it io n -10 -8 -6 -4 -2 0 50 100 pH 7.0 pH 5.2 Best-fit values Bottom Top LogIC50 IC50 Span pH 5.2 100.6 5.238 -3.439 0.0003638 -95.31 pH 7.0 115.6 1.842 -3.569 0.0002700 -113.8

(16)

log [ ] (M) % i m ig lu c e ra s e i n h ib it io n -12 -10 -8 -6 -4 0 50 100 pH 5.2 pH 7.0 Best-fit values Bottom Top LogIC50 IC50 Span pH 5.2 100.3 0.7227 -5.958 1.103e-006 -99.60 pH 7.0 98.46 3.044 -6.630 2.343e-007 -95.42

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