Table 3.

Inhibition of tau and Aβ₄₂ aggregation and BACE1 by compounds 27–39 (series III).

Cmpd.	n	R	In cellulo tau inhibition %a	In cellulo Aβ42 inhibition %a	hBACE1 %b or IC50c (μM)
27	3		64.5 ± 4.1	64.9 ± 4.5	5.76 ± 0.28
28	6		64.8 ± 2.2	64.2 ± 3.4	67.4% ± 11.3
29	7		70.3 ± 3.9	67.4 ± 4.1	4.07 ± 0.27
30	8		60.2 ± 2.6	66.7 ± 5.1	33.6% ± 11.1
31	3		39.5 ± 8.3	24.4 ± 3.4	34.0% ± 11.4
32	4		42.5 ± 6.3	43.2 ± 5.4	42.8% ± 12.7
33	5		55.8 ± 5.3	29.0 ± 4.5	31.5% ± 1.1
34	3		48.1 ± 7.0	25.5 ± 2.9	34.9% ± 1.8
35	4		45.1 ± 7.6	27.3 ± 3.1	29.6% ± 11.7
36	5		37.3 ± 2.7	30.4 ± 3.9	29.0% ± 6.3
37	2		57.3 ± 2.4	54.1 ± 4.6	40.9% ± 5.8
38	3		60.2 ± 3.0	55.7 ± 4.6	32.5% ± 7.8
39	4		62.8 ± 3.5	62.0 ± 4.0	47.0% ± 6.1
DP-128			68.7 ± 0.5d	77.5 ± 0.9d	–
Inh. IV			–	–	0.08 ± 0.01

^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.

^dRef. di Pietro et al.³⁸.