Penem derivates with mercapto pyrrolidine formamide benzene alkyl heterocycle

Abstract

The invention relates to a penem derivative containing sulfhydryl pyrrolidine formamide heterocyclic alkyl benzene as shown in general formula (I), and also relates to the easy hydrolysis esters of the derivative, the pharmaceutical acceptable non-toxic salts of the derivative, the isomers of the derivative, the hydrates of the derivative, as well as the hydrates of the esters or salts of the derivative; wherein, the detailed definitions of R1, R2, R3, R4, R5, R6, R7 and n are shown in the instruction book. The invention also relates to the preparation methods for the compounds in formula (I), the drug combinations containing the compounds in formula (I), as well as the purposes of the compounds in formula (1) as medicinal active substances, especially the applications of the compounds inthe preparation of drugs for curing and / or preventing infectious diseases.

Description

1. Technical field The present invention relates to penem derivatives containing mercaptopyrrolidinecarboxamide phenylalkyl heterocycles, their easily hydrolyzed esters, their pharmaceutically acceptable non-toxic salts, their isomers, their hydrates, and their esters or salts Hydrates of these compounds, preparation methods of these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds for preparing medicines for treating and / or preventing infectious diseases belong to the field of medical technology. 2. Background technology Carbapenems are new broad-spectrum, enzyme-resistant and highly effective β-lactam antibiotics developed in the 1970s. In 1976, Thiamycin, the first carbapenem antibiotic, was discovered, but it was not used clinically due to its poor chemical stability. Later, the chemical structure modification of thiamycin produced a series of carbapenem derivatives. At present, such drugs that have been marketed include...

AI Technical Summary

Problems solved by technology

Due to the continuous increase of bacterial resistance and the limitation of digestive tract absorption due to the abuse of antibiotics, the carbapenems currently on the market can only be administered as injections in clinical practice, and the clinical utilization is not high, and the antibacterial activity against MRSA Weak, can no longer meet clinical needs

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