Pyrimidine-conjugated fluoroquinolones as new potential broad-spectrum antibacterial agents was written by Tan, Yi-Min;Li, Di;Li, Fen-Fen;Fawad Ansari, Mohammad;Fang, Bo;Zhou, Cheng-He. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2022.Product Details of 70458-96-7 The following contents are mentioned in the article:
Pyrimidine-conjugated fluoroquinolones were constructed to cope with the dreadful resistance. Most of the target pyrimidine derivatives effectively suppressed the growth of the tested strains, especially, 4-aminopyrimidinyl compound 1c showed a broad antibacterial spectrum and low cytotoxicity and exhibited superior antibacterial potency against Enterococcus faecalis with a low MIC of 0.25 μg/mL to norfloxacin and ciprofloxacin. The active compound 1c with fast bactericidal potency could inhibit the formation of biofilms and showed much lower trend for the development of drug-resistance than norfloxacin and ciprofloxacin. Further exploration revealed that compound 1c could prompt ROS accumulations in bacterial cells and interact with DNA to form a DNA-1c complex, thus facilitating bacterial death. ADME anal. indicated that compound 1c possessed favorable drug-likeness and promising pharmacokinetic properties. These results demonstrated that pyrimidine-conjugated fluoroquinolones held hope as potential antibacterial candidates and deserve further study. This study involved multiple reactions and reactants, such as 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7Product Details of 70458-96-7).
1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Product Details of 70458-96-7
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics