. 2016 Aug 26;7(10):896–901. doi: 10.1021/acsmedchemlett.6b00190

Table 2. Structure–Activity Relationships for 3- and 4-Position Phenyl Modifications on Trisubstituted Hydroxylactams^a.

graphic file with name ml-2016-00190x_0007.jpg

compd	R¹	R²	LDHA IC₅₀ (μM)	LDHB IC₅₀ (μM)
15	1-morpholino	H	0.080	0.25
16	NH-THP	H	0.009	0.16
17	NH-cyclohexyl	H	0.004	0.077
18	NH-(4-F)Ph	H	0.003	0.035
19	O-THP	H	0.069	0.66
20	O-(4-F)Ph	H	0.037	0.19
21	H	cyclohexyl	0.025	0.18
22	H	1-piperazinyl	0.052	0.78
23	H	1-(4-oxetane)piperazinyl	0.047	0.39
24	H	1-(4-OMe)piperidinyl	0.016	0.075
25	H	1-piperidinyl	0.009	0.049
26	H	1-pyrrolidinyl	0.007	0.050
27	H	1-(4-acetyl)piperazinyl	0.005	0.035
28	H	1-morpholino	0.009	0.030
29-R	H	1-morpholino	0.003	0.005
30-S	H	1-morpholino	0.055	0.14

Compounds are racemic mixtures, except where indicated.

Table 2. Structure–Activity Relationships for 3- and 4-Position Phenyl Modifications on Trisubstituted Hydroxylactamsa.