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. Author manuscript; available in PMC: 2019 Dec 3.
Published in final edited form as: J Med Chem. 2019 Mar 21;62(7):3354–3366. doi: 10.1021/acs.jmedchem.8b01785

Table 2.

Antibacterial Activity against 7 Strains of A. baumannii Resistant to Polymyxin B and Colistin and 20 Worldwide 2016 and 2017 Isolates Resistant to 18 Classical Antibiotics

peptide namea peptide mass MICGM (μM)b MICGM (μM)c
With Specificity Determinants
D87(Lys1-6 Arg-1) 3033.7 0.8 nd
D84(Lys1-6 Lys-1) 2865.6 0.5 0.7
D85(Lys1-6 Orn-1) 2781.5 0.5 nd
D86(Lys1-6 Dab-1) 2697.3 1.0 1.0
D105(Lys1-6 Dap-1) 2613.1 1.2 1.0
D101(Lys1Ser26-5 Lys-1) 2824.5 0.8 1.0
D102(Lys1Ser26-5 Dab-1) 2684.3 0.7 0.6
Without Specificity Determinants
D85(K13A/K16A)-(Lys1-6 Orn-1) 2667.3 2.0 1.9
D86(K13A/K16A)-(Lys1-6 Dab-1) 2583.1 0.9 0.9
D105(K13A/K16A)-(Lys1-6 Dap-1) 2499.0 1.3 2.0
Colistin 1155.5 >28 nd
Polymyxin B 1301.6 >25 nd
a

6 Lys-1 denotes 6 Lys residues on the polar face at positions 3,7, 11, 18, 22, and 26; 5 Lys-1 denotes 5 Lys residues on polar face at positions 3, 7, 11, 18, and 22 (position 26 is substituted by Ser).

b

MIC is minimal inhibitory concentration (μM) that inhibited growth of different strains in MH medium at 37 °C after 24 h, with the MIC based on three sets of replicates; MICGM is the geometric mean of the MIC values from seven different strains of A. baumanii resistant to polymyxin B and colistin, antibiotics of last resort.

c

MICGM is the geometric mean of the MIC values for 20 worldwide 2016 and 2017 isolates resistant to 18 classical antibiotics.