The synthesis and antibacterial activity of a series of 1β-methylcarbapenems having quaternary heteroaromatic-thiomethyl groups at the C-2 position are described. Both 2-hydroxymethyl and 2-chloromethyl carbapenems (1 and 7) respectively served as the common key intermediates for the preparation of these compounds. Of these, the 4-pyridiniothiomethyl derivatives exhibited the best antibacterial properties and turned out to possess high in vivo efficacy as well.
描述了一系列具有四元杂环-
硫甲基基团在C-2位的1β-甲基碳烯类的合成及其抗菌活性。2-羟甲基和2-
氯甲基碳烯类(1和7)分别作为这些化合物的共同关键中间体。在这些化合物中,4-
吡啶基
硫甲基衍
生物表现出最佳的抗菌特性,并且在体内也显示出较高的疗效。