Computed Properties of C7H13NO2On October 31, 2020 ,《Design and synthesis of novel desfluoroquinolone-aminopyrimidine hybrids as potent anti-MRSA agents with low hERG activity》 appeared in Bioorganic Chemistry. The author of the article were Song, Runzhe; Wang, Yue; Wang, Minghui; Gao, Ruixuan; Yang, Teng; Yang, Song; Yang, Cai-Guang; Jin, Yongsheng; Zou, Siyuan; Cai, Jianfeng; Fan, Renhua; He, Qiuqin. The article conveys some information:
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. In the experimental materials used by the author, we found Ethyl 3-(dimethylamino)acrylate(cas: 924-99-2Computed Properties of C7H13NO2)
Ethyl 3-(dimethylamino)acrylate(cas: 924-99-2) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.Computed Properties of C7H13NO2
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