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. 2021 Aug 16;12(9):1478–1485. doi: 10.1021/acsmedchemlett.1c00345

Table 2. Antimicrobial Susceptibility of the Optimized NBTIs against a Panel of Gram-Positive and Gram-Negative Bacterial Pathogens.

  MIC (μg/mL)
compound 1a 2a 3a 4 5 6 7 8 9 10 11 12 13 Gepo
S. aureus (ATCC 29213) 0.125 0.031 0.008 0.031 0.008 0.008 0.008 0.004 0.008 0.031 0.008 1 0.125 0.125
E. coli (ATCC 25922) 4 2 2 2 1 0.5 0.5 0.5 1 4 2 32 32 1
E. coli D22b 2 0.125 0.125 0.25 0.062 0.062 0.031 0.016 0.25 0.5 0.125 4 16 0.125
E. coli N43c (CGSC no. 5583) 0.5 0.125 0.078 0.062 0.031 0.016 0.062 0.008 0.062 0.125 0.031 8 8 0.016
MRSA (QA-11.7)d 0.5 0.062 0.008 0.031 0.016 0.016 0.031 0.016 0.016 0.062 0.031 1 0.25 0.062
MRSA (QA-12.1)e ND ND ND 0.031 0.031 0.016 0.031 0.016 0.016 0.062 0.062 2 0.25 0.125
Klebsiella pneumoniae ND ND ND 32 16 8 8 8 64 64 32 >128 >128 8
Salmonella alachua RDK 030c (QA-1482/04) 32 16 8 8 4 2 2 1 16 16 8 >128 >128 4
Pseudomonas aeruginosa RDK 184 (DSM 939) >128 128 32 64 32 16 16 8 128 >128 64 >128 >128 8
Streptococcus agalactiae RDK 047 (QA-990/02) 1 0.5 0.125 1 2 0.25 0.5 0.25 0.25 2 0.5 64 8 ND
Enterococcus faecalis DRK 057 (ATCC 29212) 1 1 1 2 0.5 0.25 0.5 0.5 0.5 2 0.5 32 4 ND
a

Ref (31). ATCC, American Type Culture Collection; CGSC, Coli Genetic Stock Centre; QA, quality assurance; DSM, German Collection of Microorganisms and Cell Cultures; ND, not determined; Gepo, gepotidacin.

b

With a mutation in the lpxC gene that increases membrane permeability.

c

With the AcrA knockout (cell membrane efflux pump).

d

Resistant to cefoxitin, ciprofloxacin, clindamycin, erythromycin, tetracycline, thiamulin, and trimethoprim.

e

Resistant to cefoxitin, gentamicin, kanamycin, rifampicin, streptomycin, sulfamethoxazole, and tetracycline.