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. 2017 Jul 26;22(8):1254. doi: 10.3390/molecules22081254

Table 1.

The chemical structures and biological activities of DL0410 and its 50 derivatives as AChE and BuChE inhibitors.

graphic file with name molecules-22-01254-i001.jpg
Compound No. R1 R2 IC50(μM)
AChE BuChE
1-1 graphic file with name molecules-22-01254-i007.jpg graphic file with name molecules-22-01254-i007.jpg 0.096 1.25
1-2 graphic file with name molecules-22-01254-i008.jpg graphic file with name molecules-22-01254-i008.jpg 0.84 2.22
1-3 graphic file with name molecules-22-01254-i009.jpg graphic file with name molecules-22-01254-i009.jpg 1.32 5.9
1-4 graphic file with name molecules-22-01254-i010.jpg graphic file with name molecules-22-01254-i010.jpg 0.82 2.65
1-5 graphic file with name molecules-22-01254-i011.jpg graphic file with name molecules-22-01254-i013.jpg 0.41 1.88
1-6 graphic file with name molecules-22-01254-i012.jpg graphic file with name molecules-22-01254-i011.jpg 3.32 4.87
1-7 graphic file with name molecules-22-01254-i014.jpg graphic file with name molecules-22-01254-i014.jpg 49.05 36.58
1-8 graphic file with name molecules-22-01254-i015.jpg graphic file with name molecules-22-01254-i015.jpg 0.75 0.19
1-9 graphic file with name molecules-22-01254-i016.jpg graphic file with name molecules-22-01254-i016.jpg 1.18 0.74
1-10 graphic file with name molecules-22-01254-i017.jpg graphic file with name molecules-22-01254-i017.jpg 0.88 2.83
1-11 graphic file with name molecules-22-01254-i018.jpg graphic file with name molecules-22-01254-i018.jpg 0.71 2.39
1-12 graphic file with name molecules-22-01254-i019.jpg graphic file with name molecules-22-01254-i019.jpg 0.33 1.16
1-13 graphic file with name molecules-22-01254-i020.jpg graphic file with name molecules-22-01254-i020.jpg 1.43 1.94
1-14 graphic file with name molecules-22-01254-i021.jpg graphic file with name molecules-22-01254-i021.jpg 1.61 13.77
1-15 graphic file with name molecules-22-01254-i022.jpg graphic file with name molecules-22-01254-i022.jpg 0.97 0.72
1-16 graphic file with name molecules-22-01254-i023.jpg graphic file with name molecules-22-01254-i023.jpg 2.15 1.91
1-17 graphic file with name molecules-22-01254-i024.jpg graphic file with name molecules-22-01254-i024.jpg 3.33 6.56
1-18 graphic file with name molecules-22-01254-i025.jpg graphic file with name molecules-22-01254-i025.jpg 9.52 >200
1-19 graphic file with name molecules-22-01254-i026.jpg graphic file with name molecules-22-01254-i026.jpg 0.25 >200
graphic file with name molecules-22-01254-i002.jpg
Compound No. R1 R2 IC50(μM)
AChE BuChE
2-1 graphic file with name molecules-22-01254-i027.jpg graphic file with name molecules-22-01254-i027.jpg 75.54 20.72
2-2 graphic file with name molecules-22-01254-i029.jpg graphic file with name molecules-22-01254-i029.jpg 74.13 66.51
2-3 graphic file with name molecules-22-01254-i011.jpg graphic file with name molecules-22-01254-i011.jpg 0.50 3.41
2-4 graphic file with name molecules-22-01254-i013.jpg graphic file with name molecules-22-01254-i013.jpg 3.67 19.18
2-5 graphic file with name molecules-22-01254-i030.jpg graphic file with name molecules-22-01254-i030.jpg 0.19 1.64
2-6 graphic file with name molecules-22-01254-i031.jpg graphic file with name molecules-22-01254-i031.jpg 12.24 >200
2-7 graphic file with name molecules-22-01254-i022.jpg graphic file with name molecules-22-01254-i022.jpg 3.53 6.38
2-8 graphic file with name molecules-22-01254-i032.jpg graphic file with name molecules-22-01254-i032.jpg 62.27 9.11
2-9 graphic file with name molecules-22-01254-i015.jpg graphic file with name molecules-22-01254-i015.jpg 2.62 1.21
2-10 graphic file with name molecules-22-01254-i028.jpg graphic file with name molecules-22-01254-i028.jpg 3.96 2.77
graphic file with name molecules-22-01254-i003.jpg
Compound No. R1 R2 IC50(μM)
AChE BuChE
3-1 graphic file with name molecules-22-01254-i011.jpg graphic file with name molecules-22-01254-i011.jpg 4.11 4.2
3-2 graphic file with name molecules-22-01254-i022.jpg graphic file with name molecules-22-01254-i022.jpg 7.09 7.65
3-3 graphic file with name molecules-22-01254-i040.jpg graphic file with name molecules-22-01254-i040.jpg 48.53 40.00
3-4 graphic file with name molecules-22-01254-i041.jpg graphic file with name molecules-22-01254-i041.jpg 7.55 24.35
3-5 graphic file with name molecules-22-01254-i015.jpg graphic file with name molecules-22-01254-i015.jpg 3.32 1.72
graphic file with name molecules-22-01254-i004.jpg
Compound No. R1 R2 IC50(μM)
AChE BuChE
4-1 graphic file with name molecules-22-01254-i015.jpg graphic file with name molecules-22-01254-i015.jpg 4.89 6.00
4-2 graphic file with name molecules-22-01254-i032.jpg graphic file with name molecules-22-01254-i032.jpg 54.44 5.95
4-3 graphic file with name molecules-22-01254-i011.jpg graphic file with name molecules-22-01254-i011.jpg 3.07 3.09
4-4 graphic file with name molecules-22-01254-i012.jpg graphic file with name molecules-22-01254-i012.jpg 17.40 2.93
4-5 graphic file with name molecules-22-01254-i022.jpg graphic file with name molecules-22-01254-i022.jpg 15.67 16.32
graphic file with name molecules-22-01254-i005.jpg
Compound No. R IC50(μM)
AChE BuChE
5-1 O 0.89 5.68
5-2 S 3.89 3.44
5-3 graphic file with name molecules-22-01254-i042.jpg 14.08 >200
graphic file with name molecules-22-01254-i006.jpg
Compound No. R IC50(μM)
AChE BuChE
6-1 O 0.06 0.61
6-2 S 2.03 1.71
Compound No. Structure IC50(μM)
AChE BuChE
7-1 graphic file with name molecules-22-01254-i033.jpg 31.74 13.78
7-2 graphic file with name molecules-22-01254-i034.jpg 17.13 1.55
7-3 graphic file with name molecules-22-01254-i035.jpg 34.09 0.06
7-4 graphic file with name molecules-22-01254-i036.jpg 18.53 >200
7-5 graphic file with name molecules-22-01254-i037.jpg 3.35 0.20
7-6 graphic file with name molecules-22-01254-i038.jpg 0.03 0.44
7-7 graphic file with name molecules-22-01254-i039.jpg 1.42 4.79