Table 1.
Structures, antimicrobial activity (MIC, µg/mL) and hemolytic activity (% at 150 µM) of eight analogues of D2 resulting from Gly-scan.
| 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 |
| 1 | Gly | Nlys | N1Nal | N4MePhe | Nlys | N1Nal | Nlys | NNle | 4 | 4 | 16 | 32 | 42 |
| 2 | Nlys | Gly | N1Nal | N4MePhe | Nlys | N1Nal | Nlys | NNle | 16 | 8 | 16 | 64 | 48 |
| 3 | Nlys | Nlys | Gly | N4MePhe | Nlys | N1Nal | Nlys | NNle | 64 | 64 | >64 | >64 | 56 |
| 4 | Nlys | Nlys | N1Nal | Gly | Nlys | N1Nal | Nlys | NNle | 64 | 32 | >64 | >64 | 40 |
| 5 | Nlys | Nlys | N1Nal | N4MePhe | Gly | N1Nal | Nlys | NNle | 4 | 4 | 32 | 16 | 25 |
| 6 | Nlys | Nlys | N1Nal | N4MePhe | Nlys | Gly | Nlys | NNle | >64 | >64 | >64 | >64 | 6 |
| 7 | Nlys | Nlys | N1Nal | N4MePhe | Nlys | N1Nal | Gly | NNle | 8 | 4 | 16 | 16 | 85 |
| 8 | Nlys | Nlys | N1Nal | N4MePhe | Nlys | N1Nal | Nlys | Gly | 8 | 8 | 32 | 32–64 | 49 |
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.