The Design And Synthesis Of New Anti-anaerobic Quinolones

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.