. 2015 May 7;6(7):747–752. doi: 10.1021/ml500440u

Table 1. Benzylic Substitution Structure–Activity Relationship^a.

graphic file with name ml-2014-00440u_0004.jpg

#	R1	R2	R3	R4	X	ROMK IC₅₀ (μM)	hERG IC₅₀ (μM)
8	Me	H	H	H	C	0.170	2.8
9	F	H	H	H	C	0.060	2.4
10	OH	H	H	H	C	0.12	9.0
11	OMe	H	H	H	C	0.11	9.0
12	OEt	H	H	H	C	0.22	3.5
13	H	Me	H	H	C	0.19	1.3
14	H	H	Me	H	C	0.15	1.1
15	H	H	Me	Me	C	0.30	1.2
16	H	H	OH	H	C	0.070	2.2
17	H	H	OH	H	N	0.049	6.4

All compounds are racemic.

Table 1. Benzylic Substitution Structure–Activity Relationshipa.