Bacterial Antagonist

G907 is a selective antagonist of ATP-binding cassette (ABC) transporter MsbA with anti-microbial activity. G907 inhibits E. coli MsbA with an IC₅₀ value of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket.

4-(tert-Butyl)-benzhydroxamic Acid is a PqsR antagonist with IC₅₀s of 12.5 μM and 23.6 μM for E. coli and P. aeruginosa, respectively. 4-(tert-Butyl)-benzhydroxamic Acid reduces the production of the virulence factor pyocyanin in P. aeruginosa with an IC₅₀ of 87.2 μM.

Nogalamycin is an anthracyclinone antibiotic. Nogalamycin is a potent antibiotic against Gram-positive bacteria, also has cytotoxicity against certain tumor cells. Nogalamycin is produced by Streptomyces nogalater var. Nogalater. Nogalamycin selectively inhibits RNA synthesis after binding to DNA template. Nogalamycin can be used for researching anticancer.

Besifloxacin is a fluoroquinolone antimicrobial agent. Besifloxacin can inhibit cytokine production by monocytes. Besifloxacin has broad-spectrum antibacterial activity.

LasR antagonist 1 (Compound 7) is an antagonist for LasR with an IC₅₀ of 0.4 μM, that modulates the quorum sensing (QS) in the opportunistic pathogen Pseudomonas aeruginosa.

Anti-MRSA agent 5 (B14) is a potent
MRSA
agent with MIC₅₀ values of 0.38 μg/mL and has low hERG activity with an IC₅₀ values of >40 μM. Anti-MRSA agent 5 (B14) also has low cytotoxicity to mammal cells and unlikely to acquire bacterial resistance.

AM4085 is an orally active Antagonist for FmlH with an IC₅₀ of 0.19 μM. AM4085 reveals metabolic stability in mouse liver microsomes and blood plasma.

Anti-MRSA agent 26 is a potent anti-MRSA agent with MIC <0.015 μg/mL. Anti-MRSA agent 26 has superior activity against a broad range of Gram-positive pathogens and shows no cytotoxicity in three mammalian cell lines (Caco-2, DU-145 and MDCKII MDR1 cells) at 10 μM. Anti-MRSA agent 26 has a robust TAP pharmacophore and an excellent antibacterial activity in Staphylococcus aureus skin infection mice model.

2-(2-Heptenyl)-3-methyl-4(1H)-quinolone is a quinoline alkaloid found in Burkholderia sp. VY81. 2-(2-Heptenyl)-3-methyl-4(1H)-quinolone is promising for research of bacterial diseases in rice (e.g., soft rot) and other plant pathogens (e.g., Pythium ultimum, Fusarium oxysporum).