Hansa, Raj KC’s team published research in European Journal of Medicinal Chemistry in 2021-07-05 | 115843-99-7

European Journal of Medicinal Chemistry published new progress about Anilines Role: RCT (Reactant), RACT (Reactant or Reagent). 115843-99-7 belongs to class bromides-buliding-blocks, and the molecular formula is C6H4BrClFN, Application of C6H4BrClFN.

Hansa, Raj KC.; Khan, M. M. K.; Frangie, M. M.; Gilmore, D. F.; Shelton, R. S.; Savenka, A. V.; Basnakian, A. G.; Shuttleworth, S. L.; Smeltzer, M. S.; Alam, M. A. published the artcile< 4-4-(Anilinomethyl)-3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-ylbenzoic acid derivatives as potent anti-gram-positive bacterial agents>, Application of C6H4BrClFN, the main research area is anilinomethyl phenyl pyrazolyl benzoic acid preparation antibacterial cytotoxicity SAR; Antibiotics; Antimicrobial; Enterococcus; MRSA; Pyrazole; Staphylococcus aureus; Toxicity.

A collection of potent antimicrobials consisting of novel 1,3-bis-benzoic acid and trifluoromethyl Ph derived pyrazoles I [R = HO(O)C, F3C; R1 = Ph, 3-bromophenyl, 5-iodopyridin-2-yl, etc.] was synthesized and tested for antibacterial activity. The majority of trifluoromethyl Ph derivatives are highly potent growth inhibitors of Gram-pos. bacteria and showed low toxicity to human cultured cells. In particular, two compounds I [R = F3C; R1 = 3-fluoro-5-(trifluoromethyl)phenyl, 3,5-dichloro-4-fluorophenyl] were selected for addnl. studies. These compounds were highly effective against Staphylococcus aureus as shown by a low min. inhibitory concentration (MIC), a bactericidal effect in time-kill assays, moderate inhibition of biofilm formation as well as biofilm destruction and a bactericidal effect against stationary phase cells representing non-growing persister cells. Multistep resistance assays showed a very low tendency for S. aureus and Enterococcus faecalis to develop resistance through mutation. Addnl., in vivo mouse model studies showed no harmful effects at doses up to 50 mg/kg using 14 blood plasma organ toxicity markers or TUNEL assay in liver and kidney. Investigations into the mode of action by performing macromol. synthesis inhibition studies showed a broad range of inhibitory effects, suggesting targets that have a global effect on bacterial cell function.

European Journal of Medicinal Chemistry published new progress about Anilines Role: RCT (Reactant), RACT (Reactant or Reagent). 115843-99-7 belongs to class bromides-buliding-blocks, and the molecular formula is C6H4BrClFN, Application of C6H4BrClFN.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary