The study of 9,10-dihydroacridine derivatives as a new and effective molecular scaffold for antibacterial agent development

Design, synthesis and biological evaluation of biphenyl-benzamides as potent FtsZ inhibitors

“…Similar to compound with C-5 ′ mono-substitution (9), C-5 ′ and C-6 ′ di-substitution (22,23) absolutely abolished their antibacterial activity with an MIC more than 128 μg/mL in all three strains. Encouragingly, C-4 ′ and C-6 ′ di-substitution (24)(25)(26)(27)(28)(29)(30)(31)(32)(33) showed generally excellent antibacterial activity. When trifluoromethyl group was substituted at C-6 ′ position, six compounds were synthesized and evaluated.…”

“…Among them, compounds 25 and 27 exhibited exactly the same activity with an MIC of 0.031 μg/ mL against B. subtilis ATCC9372 and 0.25 μg/mL against S. aureus ATCC25923 and S. aureus ATCC29213. Unexpectedly, the antibacterial activity is completely lost when amide group was substituted at C-4' position (26), probably due to its high steric hindrance. In particular, compound 30 showed the most potent activity with an MIC of 0.016 μg/ mL against B. subtilis ATCC9372, 0.125 μg/mL against S. aureus ATCC25923 and 0.25 μg/mL against S. aureus ATCC29213.…”

“…The grids were negatively stained with a solution of 1% phosphotungstic acid for 1 min and air-dried. The grids were then digitally imaged on a Tecnai G2 Spirit transmission microscope [26].…”

“…The polymerization of SaFtsZ protein was monitored using a microtiter plate-based light-scattering (turbidity) assay [18,26]. in which changes in light scattering are reflected by corresponding changes in absorbance at 340 nm.…”