Table 1.

Biochemical profile of compounds 1–4^[a].

Cpd	R	R1	R2	R3	R4	R5	R6	LSD1, IC50 (μM)	% inhibition at 100 μM
									MAO A	MAO B
1a[b]								0.019 ± 0.004	97%	NI[c]
1b								0.106 ± 0.020	96%	37%
1c								0.024 ± 0.004	96%	50%
1d								0.029 ± 0.005	95%	NI
1e								0.051 ± 0.008	2%	8%
1f								0.054 ± 0.010	96%	33%
1g								0.038 ± 0.009	98%	48%
1h								0.043 ± 0.010	89%	17%
2a[d]			H					0.149 ± 0.028	94%	1%
2b[e]		meta	H					18.1 ± 2.9
2c			H					0.459 ± 0.090
2d			H					0.230 ± 0.042
2e			Br					0.080 ± 0.026	71%	29%
2f			H					0.236 ± 0.039
2g			H					0.130 ± 0.025	87%	42%
2h			H					0.280 ± 0.052
2i			H					0.173 ± 0.028
2j			H					0.767 ± 0.104
2k			H					0.190 ± 0.030
2l			H					0.083 ± 0.012
2m			H					0.400 ± 0.072
2n			H					0.236 ± 0.040
2o			H					0.581 ± 0.071
3a				H	H		H	0.090 ± 0.012	37%	8%
3b[f]				H			H	0.075 ± 0.011	76%	78%
3c				H			H	0.089 ± 0.010	69%	55%
3d[f]				H		H	H	0.043 ± 0.010	46%	NI
3e[f]				H			H	0.307 ± 0.069
3f[f]				H			H	0.061 ± 0.011	21%	17%
3g[f]				H			H	0.089 ± 0.020	5%	13%
3h				H			H	0.143 ± 0.028
3i				H			H	0.073 ± 0.011
3j					H	H	H	0.146 ± 0.022	72%	17%
3k					H	Br	H	0.159 ± 0.034	94%	NI
3l					H		H	0.135 ± 0.029
3m					H	H		3.9 ± 0.2
3n					H	H		1.7 ± 0.05
4a								10.8 ± 1.1
4b								56.2 ± 7.8
4c								NI
4d								NI
4e								NI
4f								NI
4g								NI
4h								NI
4i								NI
TCP								11.2 ± 1.8	79%	85%

^[a]Data represent mean values of at least two separate experiments in duplicate.

^[b]Ref. ^[13a], added for comparison.

^[c]NI, no inhibition.

^[d]Reff. ^{[13b, 19]}, added for comparison; compounds 2a,c-o have the Z-aminoacylamino substituent inserted at the C4 position of the TCP phenyl ring.

^[e]C3-substituted regioisomer of 2a.

^[f]Ref. ^[14], added for comparison.