Yang, Ping; Luo, Jia-Bao; Wang, Zi-Zhou; Zhang, Li-Lei; Xie, Xiao-Bao; Shi, Qing-Shan; Zhang, Xin-Guo published the artcile< Synthesis and in vitro antibacterial activity of N-acylarylhydrazone-ciprofloxacin hybrids as novel fluoroquinolone derivatives>, Recommanded Product: Thiazole-5-carboxyaldehyde, the main research area is acylarylhydrazone ciprofloxacin hybrid diastereoselective preparation mol docking antibacterial.
Twelve novel fluoroquinolone derivatives I [R = 3,4-di-HOC6H3, 2,3-di-FC6H3, 2,5-di-FC6H3, etc.] were rationally designed and synthesized by introducing N-acylarylhydrazone to the C-7 position of ciprofloxacin. Antibacterial evaluation revealed that compound I [R = (E)-2,6-di-FC6H3CH=CH] was over 4-folds more potent than ciprofloxacin against S. aureus, with a MIC value ≤0.125μg/mL. Compound I [R = (E)-4-BrC6H4CH=CH] showed activity against methicillin-resistant S. aureus (MRSA) with a MIC value of 32μg/mL. Time-killing assays showed that compound I [R = (E)-4-BrC6H4CH=CH] eradicated S. aureus in 4 h and E. coli in 2 h. Compound I [R = (E)-4-BrC6H4CH=CH] had a high affinity toward DNA topoisomerase IV, with a least binding energy of -9.9 kcal/mol, which was better than ciprofloxacin (-8.0 kcal/mol). The binding modes of compound I [R = (E)-4-BrC6H4CH=CH] to DNA topoisomerase IV differed from that of ciprofloxacin. Mol. dynamics simulation results support that the interaction between the receptor 3rae and the compound I [R = (E)-4-BrC6H4CH=CH] was stable. Besides, cytotoxicity and hemolysis assays demonstrated that compound I [R = (E)-4-BrC6H4CH=CH] and I [R = (E)-2,6-di-FC6H3CH=CH] had negligible risks of toxic effects.
Journal of Molecular Structure published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Recommanded Product: Thiazole-5-carboxyaldehyde.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica