In the original article, there was a mistake in Table 1 as published. The structure of SPR206 was partially incorrect. In the correct structure, R(FA) is (3S)-4-amino-3-(3-chlorophenyl)butanoyl, R1 is absent, and R3 is Dap+. The corrected Table 1 appears below.
Table 1.
The structures of polymyxin B, colistin, and the novel polymyxin derivatives that display improved efficacy in animal infection models (compounds 4-10)a,b.
| Compound | R (FA) | R1 | R2 | R3 | R4 | R5 | R6 | R7 | R8 | R9 | R10 | |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 1 | Polymyxin B (PMB) | Methyloctanoyl/methylheptanoyl | -Dab+ | -Thr | -Dab+ | -cy[Dab | -Dab+ | -DPhe | -Leu | -Dab+ | -Dab+ | -Thr] |
| 2 | Colistin (polymyxin E) | Methyloctanoyl/methylheptanoyl | -Dab+ | -Thr | -Dab+ | -cy[Dab | -Dab+ | -DLeu | -Leu | -Dab+ | -Dab+ | -Thr] |
| 3 | CB-182,804 | 2-chloro-phenylamino-carbonyl | -Dab+ | -Thr | -Dab+ | -cy[Dab | -Dab+ | -DPhe | -Leu | -Dab+ | -Dab+ | -Thr] |
| 4 | FADDI-002 | Octanoyl | -Dab+ | -Thr | -Dab+ | -cy[Dab | -Dab+ | -DPhe | -Ada | -Dab+ | -Dab+ | -Thr] |
| 5 | FADDI-287 | Octanoyl | -Dab+ | -Thr | -Dap+ | -cy[Dab | -Dab+ | -DLeu | -Abu | -Dab+ | -Dab+ | -Thr] |
| 6 | CA824 | (S)-1-(2-methylpropyl)-piperazine-2-carbonyl+ | – | -Thr | -Dab+ | -cy[Dab | -Dab+ | -DPhe | -Leu | -Dab+ | -Dab+ | -Thr] |
| 7 | SPR206 | (3S)-4-amino-3-(3-chlorophenyl)butanoyl | – | -Thr | -Dap+ | -cy[Dab | -Dab+ | -DPhe | -Leu | -Dab+ | -Dab+ | -Thr] |
| 8 | MicuRx-12 | 3-(2,2-dimethyl-butanoyloxy)-propanoyl (ester bond) | -Dab+ | -Thr | -Dab+ | -cy[Dab | -Dab+ | -DPhe | -Leu | -Dab+ | -Dab+ | -Thr] |
| 9 | NAB739 | Octanoyl | – | -Thr | -DSer | -cy[Dab | -Dab+ | -DPhe | -Leu | -Dab+ | -Dab+ | -Thr] |
| 10 | NAB815 | Octanoyl | -Dab+ | -Thr | -DThr | -cy[Dab | -Dab+ | -DPhe | -Leu | -Abu | -Dab+ | -Thr] |
| 11 | SPR741 (NAB741) | Acetyl | – | -Thr | -DSer | -cy[Dab | -Dab+ | -DPhe | -Leu | -Dab+ | -Dab+ | -Thr] |
The structure of one discontinued derivative (compound 3) as well as that of the potentiator compound SPR741 (NAB741) are also shown.
Amino acyl residues that differ from those in polymyxin B are boxed.
Abu, aminobutyryl; Ada, aminodecanoyl; Dap, diaminopropionyl; cy, cyclic portion indicated with brackets; Dab, diaminobutyryl; FA, fatty acyl.
The authors apologize for this error and state that this does not change the scientific conclusions of the article in any way. The original article has been updated.