Table 1.

Inhibition of tau and Aβ₄₂ aggregation and BACE1 by compounds 1–16 (series I).

Cmpd.	n	R	In cellulo tau inhibition %a	In cellulo Aβ42 inhibition %a	hBACE1 %b or IC50c (μM)
1	2		58.1 ± 4.8	40.7 ± 4.3	1.58 ± 0.15
2	5		ndd	ndd	8.07 ± 0.15
3	6		37.6 ± 2.4	29.7 ± 4.0	7.31 ± 0.24
4	7		46.4 ± 5.9	58.8 ± 4.2	1.31 ± 0.06
5	8		52.7 ± 5.7	61.8 ± 4.1	2.29 ± 0.13
6	2		54.6 ± 6.2	64.8 ± 3.4	67.4% ± 4.8
7	3		39.7 ± 3.8	48.3 ± 4.2	5.82 ± 0.34
8	4		45.1 ± 5.1	54.5 ± 3.8	19.66 ± 1.54
9	5		44.8 ± 5.6	48.0 ± 4.0	23.38 ± 1.60
10	2		43.8 ± 5.6	18.1 ± 2.7	19.49 ± 1.18
11	3		32.5 ± 5.2	16.3 ± 3.3	54.2% ± 8.1
12	5		39.2 ± 4.5	41.4 ± 1.3	50.6% ± 10.0
13	2		52.7 ± 4.2	24.3 ± 3.0	6.73 ± 0.47
14	2		34.9 ± 5.6	32.0 ± 3.7	8.31 ± 0.51
15	3		58.9 ± 3.0	39.3 ± 3.7	60.2% ± 2.9
16	4		62.9 ± 3.5	57.2 ± 4.9	56.4% ± 6.3

^aThe percent of inhibition at 10 µM (mean of three experiments ± SEM).

^bThe percent of inhibition at 10 µM (mean of three experiments ± SD).

^cMean of three experiments ± SEM.

^dNot determined.