新型抗厌氧菌喹诺酮类化合物的设计与合成

【作者】 李冕；

【导师】 郭彦春；

【作者基本信息】 郑州大学 ， 有机化学， 2000， 硕士

【摘要】 喹诺酮类药物具有广谱、高效、口服吸收良好等特点，因而在临床上得到广泛的应用，但喹诺酮类药物也存在固有的毒副作用。为了进一步提高疗效，尽可能地降低副作用，我们设计合成了七个8-位喹诺酮类化合物，以增加药物分子对细胞的渗透性，相对降低其毒性。 另外，我们分别在喹诺酮主环7-位取代哌嗪4-位上和3-位羧基上，分别引入2-甲基-5-硝基-1-乙基咪唑，形成新的“潜药”，以提高药物的抗菌谱和疗效。 在上述研究中，采用PTC反应，提高了反应效率，缩短了反应时间，共设计合成了13个新喹诺酮化合物，并通过了IR、HNMR、元素分析的检测，证明合成的新化合物结构正确。更多还原

【Abstract】 A bstractThe quinolone anti-bacterials are widely usedclinically because of their strong anti-bacteria, widespectrum, high curative effect and good absorption.However, the quinolone drugs have usuaIly someside’ effects. Recent researches are fOcused on thestructural reform of 7,8 position of Quinolone andannex on position 3, in order to develop highereffciency drugs. In this paper, seven newQuino1one compounds which was substituted byclllorine atom on position 8 of tlle main ring, weredesigned and synthesized in order to reduce theserious drawback side effect and toxicity, and toincrease the curative effect. Stronger permeabilityof the new drug molecu[es to the cells are alsoexpected.By attaching 2-methyl-5-nitLO-l -imidazolylethyl group on the nitrogen atom of the piperazinesection on position 7 or the carboxylic group onposition 3 of the quinolone, some new"latent-antibactericals" were also synthesized inorder to illcrease the anti-bacteria spectrum and thecurative effects.Phase transfer catalytic method was used in thesynthetic procedure which showed a remarkablereducing of time (from 72h to l2h) and higheffciency. TotalIy l3 new quinolone derivativeswere obtained and characterized by IR, HNMR andelelnentaI analysis. Tlle results obtained are ingood accordance with the structures required.更多还原