CAJ | 학술논문

目的研究硫酸头孢匹罗类似物的合成及其抗菌活性.方法以7-氨基头孢烷酸(7-ACA)为原料,在三乙胺催化下与苯并噻唑硫醇活性酯(MAEM)缩合得头孢噻肟酸,然后在KI作用下与取代吡啶进行3-位取代反应,最后硫酸成盐得目标化合物,并通过平皿二倍稀释法对它们的体外抗菌活性进行评价.结果合成的12个目标化合物均未见文献报道,其结构经MS,IR和~1H-NMR确证.结论初步体外抗菌活性实验结果表明,化合物1a对革兰阴性菌的活性总体上与硫酸头孢匹罗相当,特别是对大肠埃希菌和铜绿假单胞菌的活性优于硫酸头孢匹罗.
목적 연구류산두포필라유사물적합성급기항균활성.방법 이7-안기두포완산(7-ACA)위원료,재삼을알최화하여분병새서류순활성지(MAEM)축합득두포새우산,연후재KI작용하여취대필정진행3-위취대반응,최후류산성염득목표화합물,병통과평명이배희석법대타문적체외항균활성진행평개.결과 합성적12개목표화합물균미견문헌보도,기결구경MS,IR화~1H-NMR학증.결론 초보체외항균활성실험결과표명,화합물1a대혁란음성균적활성총체상여류산두포필라상당,특별시대대장애희균화동록가단포균적활성우우류산두포필라.
Objective To study the synthesis and antibacterial activity of cefpirome sulfate analogues. Methods Beginning with 7-ACA, the target compounds were obtained by consendation with MAEM in presence of Et_3N, 3-substituion with substituted pyridine using KI as catalyst, and salt formation of sulfate. Their antibacterial activities in vitro were evaluated by double broth dilution method. Results 12 new compounds were synthesized, and their structures were confirmed by MS, IR and ~1H-NMR. Conclusion The preliminary results of antibacterial activity in vitro showed that compound la possessed approximately equivalent antibacterial activity against Gramnegative bacteria to cefpirome sulfate.