Skip to main content
. 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 Hydroxylactamsa.

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
a

Compounds are racemic mixtures, except where indicated.