158183-05-2Relevant articles and documents
PRODRUG INHIBITORS
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Paragraph 00160; 00162, (2020/10/20)
Provided herein are compounds useful as metallo-β-lactamase (MBL) inhibitors. The compounds have a formula A–B, where A is a β-lactam antibiotic moiety comprising a bridging methylene (-CH2-) covalently attached to -B; and B is a latent MBL inhibitor. Also provided are formulations comprising such compounds; as well as such compounds or formulations for use as a medicament. The compounds and formulations may be used in the treatment of antibiotic resistance, bacterial infection. The compounds and formulations may be used in the inhibition of a bacterial MBL.
Method for synthesizing 2-Mercaptobenzothiazolyl-(Z)-(2-aminothiazol-4-yl)-2-(tert-butoxycarbonyl) isopropoxyiminoacetate
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Paragraph 0028-0033, (2017/07/21)
The invention relates to a method for synthesizing 2-Mercaptobenzothiazolyl-(Z)-(2-aminothiazol-4-yl)-2-(tert-butoxycarbonyl) isopropoxyiminoacetate and belongs to the technical field of preparation of ceftazidime intermediates. 2-(2-aminothiazole-4-yl)-2-acetic acid and dibenzothiazyl disulfide (DM) are used as raw materials, a dichloromethane and acetonitrile mixed solution serves as a solvent, catalysts pyridine and triethylamine are sequentially added, triethyl phosphite is used as a condensation agent to perform reaction, and suction filtration and drying are performed after reaction is completed to obtain the 2-Mercaptobenzothiazolyl-(Z)-(2-aminothiazol-4-yl)-2-(tert-butoxycarbonyl) isopropoxyiminoacetate. The process is simple, mild in condition, low in cost and high in reaction yield, and the prepared target product is high in quality and purity and suitable for mass production.
