Table 3.
Structures, antimicrobial (MIC, µg/mL), and hemolytic activity (% at 150 µM) of l- (D2L), d- (D2D), retro- (D2R), and peptide–peptoid hybrid analogues (13–16) of D2.
| ID | SEQUENCE a | MIC | HA f | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| MSSP b | MRSP c | SA d | PA e | ||||||||||
| D2 | Nlys | Nlys | N1Nal | N4MePhe | Nlys | N1Nal | Nlys | NNle | 2–4 | 4 | 8 | 16 | 24 |
| D2L | Lys | Lys | 1Nal | Phe | Lys | 1Nal | Lys | Nle | 16 | 8 | 32 | 16 | 35 |
| D2D | lys | lys | 1nal | phe | lys | 1nal | lys | nle | 1–4 | 4 | 4 | 4 | 35 |
| D2R | Nle | Lys | 1Nal | Lys | Phe | 1Nal | Lys | Lys | 16 | 4 | 32 | 32–64 | 23 |
| 13 | Nlys | Nlys | N1Nal | N4MePhe | lys | 1nal | lys | nle | 4 | 4 | 8 | 8 | 34 |
| 14 | lys | lys | 1nal | phe | Nlys | N1Nal | Nlys | NNle | 4 | 4 | 16 | 64 | 5 |
| 15 | Nlys | Nlys | 1nal | phe | Nlys | 1nal | Nlys | nle | 4 | 4 | 32 | >64 | 6 |
| 16 | lys | lys | N1Nal | N4MePhe | lys | N1Nal | lys | NNle | 4 | 4 | 16 | 64 | 4 |
a Products synthesized as C-terminal amides; b Methicillin sensitive Staphylococcus pseudintermedius (26916); c Methicillin resistant Staphylococcus pseudintermedius, (C22963); d Staphylococcus aureus (ATCC 29213); e Pseudomonas aeruginosa (ATCC 27853); f Percentage of hemolysis at 150 µM.