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. 2019 Feb 7;62(5):2521–2540. doi: 10.1021/acs.jmedchem.8b01854

Table 2. Pleuromutilins with Other Boron Heterocycles Linked via C(14).

graphic file with name jm-2018-018544_0007.jpg

ID P Q–R R8 Wolbachia infected C6/36 cells (wAlb) EC50 (nM) Wolbachia infected LDW1 cells (wMel) EC50 (nM)
40 CH3SO2N N=CH H 9 0.8
41 CH3N N=CH H 14.8 1.5
42 CH3C(=O)N N=CH H 4 0.2
43 Boc-N N=CH H 0.7 0.2
44 HN N=CH H 3.5 2.7
45 CH3OC(=O)N N=CH H 1.5 0.3
46 O N=CH H 14.2 5.1
47 CH3SO2N N=CH 8-F 240 6.3
48 CH3N N=CH 8-F 172 11
49 CH3C(=O)N N=CH 8-F 107 NTa
50 CH3OC(=O)N N=CH 8-F 164 1.3
51 O N=CH 8-F 329 27
52 CH3C(=O)N N=CH 8-CH3 26.1 NT
53 O CH2CH2 H >1000 NT
a

NT = not tested.