Zhang, Nan published the artcileModification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci, Synthetic Route of 74317-85-4, the main research area is vancomycin resistant Enterococci 5 methylphenanthridium benzothiazoles FtsZ inhibitors; Antibacterial activity; Benzothiazolyl-5-methylphenanthridium; FtsZ inhibitors; Indolyl-5-methylphenanthridium; Mechanism of action.
The death caused by pathogenic bacteria has always been a severe threat to mankind. The prevalence of drug resistance among bacteria underscores an urgent goal for new antibacterial agents with novel mode of action. Here we first designed and synthesized a class of benzothiazolyl-5-methylphenanthridium derivatives and evaluated their antibacterial activity. On this basis, we further designed and synthesized another class of novel indolyl-5-methylphenanthridium derivatives by optimizing the benzothiazolyl-5-methylphenanthridium core and evaluated their antibacterial activity targeting the bacterial cell division protein FtsZ. The results showed that the indolyl-5-methylphenanthridium derivatives had greatly improved activity against various drug-resistant bacterial strains including methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus (VRE). Among them, compound C5 displayed excellent antibacterial activity against susceptible (MIC = 1μg/mL), methicillin-resistant and clin. isolated S. aureus (MIC = 2μg/mL). With low hemolytic activity towards mice red blood cells, C5 exhibited good antibacterial effect in vivo in preliminary pharmacodynamic assay. More importantly, C5 was difficult to induce bacterial resistance. Further mechanism studies proved that C5 could inhibit bacterial cell division by promoting FtsZ polymerization, leading to disorderly polymerization and disordered knots. Therefore, our findings suggest that this class of novel indolyl-5-methylphenanthridium derivatives are promising for future antibacterial agents.
European Journal of Medicinal Chemistry published new progress about Antibacterial agents. 74317-85-4 belongs to class bromides-buliding-blocks, name is 2-Bromo-4-methoxybenzoic acid, and the molecular formula is C8H7BrO3, Synthetic Route of 74317-85-4.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary