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. 2010 Apr 1;18(7):2651–2663. doi: 10.1016/j.bmc.2010.02.026

Table 1.

Percentage inhibition of Escherichia coli MurG and Mycobacterium tuberculosis galactosyl transferase by compounds 13–25, at 1 mM concentration

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R1 R2 R3 linker E. coli MurG Mt GTase
13a Ph N-Phenyl succinimide Gly NT NT
13b 2-MeOPh N-Phenyl succinimide Gly 85 0
13c 2,3-(MeO)2Ph N-Phenyl succinimide Gly 0 0
13e Ethane-1,2-diol N-Phenyl succinimide Gly 0 0
14a Ph -CO2Me α–CO2Me Gly 0 NT
14b 2-MeOPh -CO2Me α–CO2Me Gly 32 0
15b 2-MeOPh -CO2Me Bicyclic Gly 22 0
15e Ethane-1,2-diol -CO2Me Bicyclic Gly 27 NT
16a Ph -CO2Me Bicyclic Gly 0 80
16b 2-MeOPh -CO2Me Bicyclic Gly 0 0
16c 2,3-(MeO)2Ph -CO2Me Bicyclic Gly 0 NT
16d 3,4-(MeO)2Ph -CO2Me Bicyclic Gly 26 0
19 2-MeOPh N-Phenyl succinimide Sar 31 NT
20a 2-MeOPh N-Phenyl succinimide Pro 0 0
20b 2-MeOPh -CO2Me β–CO2Me Pro 0 0
20c 2-MeOPh -CO2Me α–CO2Me Pro 22 0
20d Ethane-1,2-diol N-Ethyl succinimide Pro 0 0
24 2-MeOPh N-Phenyl succinimide C3 17 0
25 2-MeOPh N-Phenyl succinimide C4 15 0

Linkers: glycine (Gly), sarcosine (Sar), proline (Pro), C-3 diester (C3), C-4 diester (C4). NT, not tested. Assays carried out as described in Section 4.