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. 2020 Sep 14;63(20):11707–11724. doi: 10.1021/acs.jmedchem.0c00856

Table 2. Antibacterial Activity of Lectin Targeted Conjugates 2231, 20, and Ciprofloxacin (3) against a Panel of Bacterial Organisms. LecA-targeting galactosides were generally more active than the LecB-targeting conjugates. A shorter linker length on the side of the antibiotic led to increased antimicrobial activitya.

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  target: LecA
target: LecB
references
compound 22 23 24 25 26 27 28 29 30 31 20 3
molecular mass [g/mol] 739.8 753.8 753.8 767.8 767.8 781.9 781.9 795.9 761.8 775.9 369.4 331.3
linker length n/m 1/0 1/1 2/0 2/1 3/0 3/1 4/0 4/1 -/0 -/1 0  
 
test organism MIC [μg/mL]
E. coli K12 MG1655 2 8–16 2 16 1–2 16 2–4 16 8–16 16 n.d. <0.125
E. coli DSM 1116 2–4 16 2–4 32 2–32 4–32 4–32 4–32 16–32 32 n.d. <0.125
S. carnosus DSM 20501 32 64 32 >64 16 64 8 ≥64 >64 >64 n.d. <0.125
P. aeruginosa PA14 wt 16 ≥64 8–16 >64 8–16 >64 32 >64 64 >64 2–4 0.025–0.1
P. aeruginosa PA14 wt + 1 μg/mL PMBN 4–16 16–64 8–16 32–64 4 32–64 2–8 32–64 64 64 0.025–0.5 0.025
P. aeruginosa PA14 ΔlecA 16–32 ≥64 8–16 >64 8–16 >64 32 >64 ≥64 >64 4–8 0.05–0.08
P. aeruginosa PA14 ΔlecB 16–32 ≥64 8–32 >64 8–16 >64 32–64 >64 64 >64 4 0.05–0.08
P. aeruginosa PAO1 wt 16–32 >64 16 >64 16–32 >64 32–64 >64 ≥64 >64 4–8 0.025–0.08
P. aeruginosa PAO1 wt + 1 μg/mL PMBN 4–8 32–64 4–8 32–64 4–8 32–64 8–16 32–64 32–64 ≥64 1–2 0.025–0.05
a

Data is presented as minimal inhibitory concentration (MIC) range from at least three independent experiments. Molar MIC is given in Table S2. n.d. = not determined.