5′-去氧-5′-N-[3-(2-羟基苯)丙烯酰基]氨基腺苷的设计与合成

Design and synthesis of 5′-deoxy-5′-N-[3-(2-hydroxy)phenpropyleneacyl]aminoadenosine

分枝杆菌生长素是结核分枝杆菌生长和毒性的关键性因素。MbtA酶是催化生物合成分枝杆菌生长素的关键性酶,现已成为新型抗结核药物研究的重要靶点。以水杨醛、嘌呤核苷为原料,经过麦克尔加成反应、羟醛缩合等一系列的反应,设计合成了新型核苷类标题化合物。目标化合物采用IR、MS、1HNMR和13CNMR测试技术对其结构进行了表征。

Mycobactins are the critical factors for the growth and virulence of M.tuberculosis.Biosynthesis of mycobactin begins with an adenylate-forming enzyme,MbtA,which has emerged as an attractive target for the development of anti-TB agents.A new compound 5′-deoxy-5′-N-[3-（2-hydroxy）phenpropyleneacyl] aminoadenosine,which was designed to be an inhibitor of MbtA,was synthesized from the starting materials salicylaldehyde and adenosine via a series of reactions such as the Michael addition and condensation reactions.The structure of the compound was determined by 1HNMR,13CNMR,IR and MS/ESI.The biological activity of this compound was also investigated.