Song, Runzhe published the artcileDesign and synthesis of novel desfluoroquinolone-aminopyrimidine hybrids as potent anti-MRSA agents with low hERG activity, Quality Control of 924-99-2, the publication is Bioorganic Chemistry (2020), 104176, database is CAplus and MEDLINE.
The desfluoroquinolone-based hybrids with involvement of C-7 aminopyrimidine functional group were designed and synthesized. The biol. results showed majority of these hybrids still demonstrated potent anti-MRSA activity with MIC values between 0.38 and 1.5μg/mL, despite the lack of the typical C-6 fluorine atom. Particularly, the most active 1-cyclopropyl-7-((4-(3,4-dimethylphenoxy)pyrimidin-2-yl) amino)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid exhibited activities at submicromolar concentrations against a panel of MRSA strains including vancomycin-intermediate strains, levofloxacin-resistant isolates, and linezolid-resistant isolates, etc. As expected, it also displayed highly selective toxicity toward bacterial cells and low hERG inhibition. Further resistance development study indicated MRSA is unlikely acquired resistance against 1-cyclopropyl-7-((4-(3,4-dimethylphenoxy)pyrimidin-2-yl)amino)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid. The docking study revealed that two hydrogen bonds were formed between the C-7 substituent and the surrounding DNA bases, which contributed to resistance by reducing the dependence on the magnesium-water bridge interactions with topoisomerase IV. These indicated a promising strategy for developing new antibiotic quinolones to combat multidrug resistance and cardiotoxicity was resulted.
Bioorganic Chemistry published new progress about 924-99-2. 924-99-2 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Amine,Aliphatic hydrocarbon chain,Ester, name is Ethyl 3-(dimethylamino)acrylate, and the molecular formula is C9H7NO3, Quality Control of 924-99-2.
Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics