Penem derivates containing sulfhydryl pyrrolidine vinyl heterocycle

Abstract

The invention pertains to the technical field of medicine and particularly relates to a penem derivative which contains sulfhydryl pyrrolidine vinyl heterocyclic and is shown as general formula (I), and pharmaceutically acceptable salts, easily hydrolysable ester and isomers of the derivative; wherein, R<1>, R<2>, R<3>, R<4>, X and Y are defined as the specification. The invention also relates toa preparation method of the compounds, medicine composition containing the compounds as well as application of the compounds to the preparation of medicines treating and / or preventing infectious diseases.

Description

1. Technical field The present invention belongs to the technical field of medicine, and specifically relates to penem derivatives containing mercaptopyrrolidine vinyl heterocycles, pharmaceutically acceptable salts thereof, easily hydrolyzed esters thereof, and isomers thereof, and methods for preparing these compounds, including these The pharmaceutical composition of the compounds, and the use of these compounds in the preparation of medicines for treating and / or preventing infectious diseases. 2. Background technology Penem 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 double bond of cephalosporin...

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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