Table 3. Position 9 Modification of Peptides.
| Antibacterial
activity (μg/mL) |
% Hemolysis | ||||||
|---|---|---|---|---|---|---|---|
| Compound | E. coli ATCC 25922 | E. coli (MCR-1) | K. pneumoniae ATCC 13883 | A. baumannii ATCC 17961 | P. aeruginosa PAO1 | S. aureus USA300 | Sheep red blood cells |
| LL(Leu9)-NH2 (42) | 4 | 8 | 8 | 4 | 8 | >32 | <0.1 |
| LL(Phe9)-NH2 (43) | 4 | 4 | 8 | 4 | 8 | >32 | 0.6 |
| LL(Met9)-NH2 (44) | 4 | 4 | 4 | 4 | 4 | >32 | 0.6 |
| LL(Trp9)-NH2 (45) | 4 | 4 | 4 | 4 | 16 | >32 | 2.1 |
| LL(Ser9)-NH2 (46) | 4 | 8 | 4 | 8 | 4 | >32 | <0.1 |
| LL(Asn9)-NH2 (47) | 8 | 8 | 8–16 | 16 | 8 | >32 | <0.1 |
| LL(Gln9)-NH2 (48) | 4 | 8 | 4 | 8 | 4 | >32 | 0.6 |
| LL(MeAbu9)-NH2 (49) | 4 | 4 | 4 | 2 | 4 | >32 | <0.1 |
| LL(Dap[Alloc]9)-NH2 (50) | 2 | 4 | 4 | 4 | 8 | >32 | <0.1 |
| LL(Glu[OAll]9)-NH2 (51) | 16 | 16 | >32 | 16 | >32 | >32 | <0.1 |
| LL(Dap9)-NH2 (52) | 8 | 8 | 32 | 16 | 18 | >32 | <0.1 |
| Δ12LB (Leu9)-NH2 (53) | 4 | 4 | 4 | 4 | 8 | >32 | 1.1 |
| Δ12LB (Phe9)-NH2 (54) | 2 | 2–4 | 2–4 | 4 | 4 | >32 | 1.1 |
| Δ12LB (Met9)-NH2 (55) | 4 | 4 | 4 | 4 | 4 | >32 | 0.7 |
| Δ12LB (Trp9)-NH2 (56) | 4 | 4 | 8 | 4 | 8 | 16 | 0.8 |
| Δ12LB (Ser9)-NH2 (57) | 4 | 8 | 4 | 8 | 2 | >32 | 0.6 |
| Δ12LB (Asn9)-NH2 (58) | 8 | 8 | 16 | 16 | 2 | >32 | 0.2 |
| Δ12LB (Gln9)-NH2 (59) | 8 | 8 | 16 | 16 | 2 | >32 | 0.5 |
| Δ12LB (MeAbu9)-NH2 (60) | 4 | 4 | 2 | 2 | 4 | >32 | 0.7 |
| Δ12LB (Dap[Alloc]9)-NH2 (61) | 4 | 4 | 2 | 2 | 4 | >32 | <0.1 |
| Δ12LB (Glu[OAll]9)-NH2 (62) | 4 | 8 | 4 | 8 | 2 | >32 | 1.1 |
| Δ12LB (Asp9)-NH2 (63) | >32 | >32 | >32 | >32 | 4 | >32 | 0.3 |
| Δ12LB (Dap9)-NH2 (64) | 8 | 8 | >32 | 16 | 4 | >32 | 0.3 |