Penem derivative containing sulfhydryl pyrrolidine formamido triazine

Abstract

The invention belongs to the medicine technology field, which more particularly relates to an ertapenem compound containing hydrosulphonyl pyrrolidine formamide triazine, the pharmaceutically acceptable salt thereof, the ester which is easy to be hydrolyzed, the isomer thereof, the hydrate thereof and the hydrate of ester or salt thereof shown in the formula (I) and a preparing method of the compound shown in the formula (I); wherein, the definitions of R<1>, R<2>, R<3>, R<4>, R<5> and R<6> are described in the specification. The invention also relates to preparing methods of compounds and the drug combination containing the compounds and the applications of the compounds in preparing the medicine for treating or preventing infectious diseases.

Description

1. Technical field The invention belongs to the technical field of medicine, and in particular relates to penem compounds containing mercaptopyrrolidine carboxamidotriazine, their pharmaceutically acceptable salts, their easily hydrolyzed esters, their isomers, their hydrates, and their esters or Hydrates of salts, preparation methods of these compounds, pharmaceutical compositions containing these compounds, and uses of these compounds in the preparation of medicaments for treating and / or preventing infectious diseases. 2. Background technology Carbapenem antibiotics are a class of β-lactam antibiotics developed in the 1970s. It has attracted much attention because of its broad antibacterial spectrum, strong antibacterial activity, and stability to β-lactamase. Its structural feature is that the sulfur at the 1-position of the penicillane core is replaced by carbon, and the 2-position has a double bond, which combines the five-membered ring of penicillin and the conjugated...

AI Technical Summary

Problems solved by technology

Due to the continuous increase of bacterial resistance due to the abuse of antibiotics, and the limitation of digestive tract absorption, the currently marketed carbapenems can only be administered as injections in clinical practice, and the clinical utilization is not high. The half-life of penem is relatively short, which can no longer meet the clinical needs

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