Antibacterial agent 307 hydrochloride

Antibacterial agent 307 (Compound 13e) (24 h) hydrochloride potently inhibits growth of gram-positive bacterial strains (S. aureus ATCC25923, S. aureus ATCC43300, E. faecalis ATCC29212, B. subtilis ATCC9372) with MIC values of 1, 2, 2, and 4 μg/mL, respectively, and exhibits weaker activity against gram-negative strains with MIC values of 16 and 32 μg/mL for E. coli ATCC25922 and P. aeruginosa ATCC27853, respectively^[1].
Antibacterial agent 307 (1-512 μg/mL; 1 h) hydrochloride exhibits low hemolytic toxicity toward sheep red blood cells, with an HC₅₀ of 95.01 μg/mL, resulting in less than 10% hemolysis at concentrations up to 64 μg/mL^[1].
Antibacterial agent 307 (1-128 μg/mL; 24 h) hydrochloride has low cytotoxicity toward LO2 human liver cells, with a CC₅₀ of 26.38 μg/mL, and a promising selectivity index of 89.21 against S. aureus ATCC25923^[1].
Antibacterial agent 307 (18 h) hydrochloride shows excellent plasma stability, maintaining an MBC of 8 μg/mL against S. aureus ATCC25923 after up to 6 h pre-incubation in 50% plasma, and retains potent bactericidal activity in mammalian fluids with MBC values of 8, 8, and 16 μg/mL in 50% plasma, 50% serum, and 50% blood, respectively^[1].
Antibacterial agent 307 (1-8 μg/mL; 24 h) hydrochloride exhibits rapid, dose-dependent bactericidal activity against S. aureus ATCC25923, reducing bacterial load by 4.51 log₁₀ CFU/mL within 8 h at 4 μg/mL and completely eradicating bacteria within 4 h at 8 μg/mL^[1].
Antibacterial agent 307 (0.5 μg/mL; 18 h per passage, 20 consecutive days) hydrochloride has a low propensity to induce resistance in S. aureus ATCC25923, as its MIC remains nearly unchanged within 17 days of serial passaging^[1].
Antibacterial agent 307 (0.5-16 μg/mL; 24 h) hydrochloride inhibits S. aureus ATCC25923 biofilm formation by up to 73.6% at 16 μg/mL and disrupts pre-formed biofilms by up to 38.0% at 16 μg/mL, demonstrating concentration-dependent anti-biofilm activity^[1].
Antibacterial agent 307 (1-8 μg/mL; 30 min) hydrochloride disrupts the membrane polarization of S. aureus ATCC25923 in a concentration-dependent manner, causing a 6.8-fold increase in DiSC₃(5) fluorescence intensity at 8 μg/mL^[1].
Antibacterial agent 307 (1-8 μg/mL; 30 min) hydrochloride increases the membrane permeability of S. aureus ATCC25923 in a concentration-dependent manner, causing a 2.6-fold increase in PI fluorescence intensity at 8 μg/mL within 24 min^[1].
Antibacterial agent 307 (1-16 μg/mL; 30 min) hydrochloride induces concentration-dependent intracellular oxidative stress in S. aureus ATCC25923, increasing ROS levels by 2-fold at 16 μg/mL relative to the control^[1].
Antibacterial agent 307 (1-16 μg/mL; 4 h) hydrochloride disrupts the membrane of S. aureus ATCC25923, causing concentration-dependent leakage of intracellular DNA and protein, with a 4.6-fold increase in extracellular DNA and 2.2-fold increase in protein leakage at 16 μg/mL relative to the control^[1].

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