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由于耐药菌的迅速增长 ,世界上许多制药公司都在积极开发新的抗菌药。唑烷酮类 ,以利奈唑胺(linezolid )的上市为标志 ,成为 3 5年来首次上市的结构全新的抗菌药。该类药物作用机制独特 ,竞争性与核糖体5 0S亚基上的P -位点相结合 ,而导致肽转移酶无法与这一位点结合 ,抑制第一个肽键的形成 ,来发挥抗菌作用。构效关系研究显示 5位碳链的最适长度是一个碳 ,N上的H为活性必需基团。 4′ -位与 5 -位取代基的脂溶性之间的平衡关系与抗菌活性有一定的关系。孟庆国和Lohray等对Brickner等报道的合成路线进行了改进
Due to the rapid growth of resistant bacteria, many pharmaceutical companies around the world are actively developing new antimicrobial agents. The oxazolidinones, marketed as linezolid, became the first brand new antimicrobials to be marketed in 35 years. The mechanism of action of these drugs is unique and competitive with the P - site on the ribosomal 50S subunit, which leads to the fact that the peptide transferase can not bind to this site and inhibits the formation of the first peptide bond to exert antimicrobial activity effect. The structure-activity relationship study shows that the optimum length of carbon chain 5 is one carbon and H on N is an active essential group. The equilibrium relationship between the 4 ’- position and the fat solubility of the 5 - substituent is related to the antibacterial activity. Meng Qingguo and Lohray et al. Improved the synthetic route reported by Brickner et al