N-(t-butoxy carbonyl ) timonacic compounds, and preparation and use thereof

Abstract

The invention relates to a class of N-(tert-butoxycarbonyl) timonacic compounds of the right general formula, and the novel N-(tert-butoxycarbonyl) timonacic compounds can inhibit not only Gram positive bacterial strains but also Gram negative bacterial strains, and the result also shows that one of the compounds has strong capability of inhibiting pseudomonas aeruginosa strains and great potential in becoming a class of thiazolidine antibacterial drugs. The invention discloses a manufacturing method of the compounds.

Description

technical field The present invention relates to a class of novel N-(tert-butoxycarbonyl) thiazolidinic acid compounds, their preparation method and their use as antibacterial drugs. Background technique Currently, heterocyclic compounds have been intensively studied due to their important properties and wide applications. Among these compounds, thiazole and thiazolidine derivatives have been widely concerned recently (A.Serganov, et al.Nature2006,42,993-1003; J.Yang, et al.J.Med.Chem.2008,51,2100 -2107.). It has been reported that 2-substituted thiazole-4(R) carboxylic acids (TCAs) prevent the induction of hepatic effects of high doses of acetaminophen (H.T.Nagasawa, et al.J.Med.Chem.1982, 25, 489-491 .). These TCAs release thiol amino acids as drugs through non-enzymatic ring opening and hydrolysis. Presumably, release of these cysteines is transported to cells by biochemical precursors of the amino acid, resulting in increased hepatic glutathione (GSH) levels. GSH is...

AI Technical Summary

Problems solved by technology

So far, people's research on thiazolidinic acid compounds has been limited to extracting and separating them from plants containing such compounds and then studying their biological activities, and there are not many reports on the targeted design and synthesis of thiazolidine acid compounds

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