Table 1.
Compounds prepared and screened as inhibitors of BaPanK
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| Yield (%) | % enzyme activitya | Yield (%) | % enzyme activitya | Yield (%) | % enzyme activitya | Yield (%) | % enzyme activitya | |||||
| α-D-Glc | 37 | (72) | 93 | 49 | (61) | 98 | 6016 | (74) | 96 | 71 | (60) | 90 |
| β-D-Glc | 38 | (85) | 95 | 50 | (88) | 91 | 61 | (91) | 99 | 72 | (80) | 104 |
| α-D-Gal | 39 | (84) | 97 | 51 | (68) | 80b | 6216 | (81) | 105 | 73 | (67) | —c |
| β-D-Gal | 40 | (82) | 4 | 52 | (54) | —c | 63 | (87) | 105 | 74 | (70) | 86 |
| α-D-Man | 41 | (86) | 84 | 53 | (62) | 108 | 64 | (80) | 94 | 75 | (76) | 105 |
| α-D-Xyl | 42 | (88) | 90 | 54 | (60) | 102 | 65 | (94) | 91 | 76 | (82) | 102 |
| β-D-Xyl | 43 | (85) | 90 | 55 | (57) | 100 | 66 | (94) | 91 | 77 | (81) | 100 |
| α-D-GlcNAc | 44 | (80) | 95 | 56 | (82) | 92 | 6716 | (90) | 102 | 78 | (83) | 109 |
| β-D-GlcNAc | 45 | (53) | 87 | 57 | (49) | 98 | 68 | (76) | 110 | 79 | (68) | —c |
| L-Ara (α/β = 1:3) | 46 | (84) | 76 | 58 | (58) | 104 | 69 | (81) | —c | 80 | (80) | 91 |
| β-D-Rib | 47 | (71) | 95 | 59 | (81) | 100 | 70 | (81) | 83 | 81 | (70) | 107 |
| D-GlcN (α/β = 1.1:1) | 48 | (48) | 93 | |||||||||
a
Assays carried out in the presence of inhibitor (1 mM), ATP (125 μM) and pantothenate (250 μM). Percentage activity is relative to the same assay carried out in the absence of inhibitor.
b
No further decrease in activity was observed when inhibitor concentration was increased to 2 mM.
c
False positives (ie. inhibition of the PK/LDH coupled enzymes) in this assay.