INSTITUTUL NAÅ¢IONAL DE CERCETARE-DEZVOLTARE - ICECHIM

3. Chemistry in medical and pharmaceutical applications - OSYNTHESIS AND ANTIBACTERIAL ACTIVITY OF QUINOLONE DERIVATIVESPINTILIE Lucia 1 , NITA Sultana 1 , CAPROIU Miron Teodor 2 ,DIACONU Alexandra 1 , NEGUT Catalina 1 , TANASE Constantin 1 , COCU Florea 11 National Institute for Chemical-Pharmaceutical Research and Development, 112 Vitan Av., 74373 Bucharest 3,Romania2Organic Chemistry Center "C.D.Nenitescu", 202 B Splaiul Independentei, Bucharest 6, Romania.The discovery of fluoroquinolones after 1980 represented a decisive step forward forchemical anti-infectious therapy. A large number of fluoroquinolones are used today inmedical practices and some of them are deemed by leading pharmacologists to be of vitalimportance to anti-infectious therapy. The research for an ideal quinolone continuesworldwide. Such a quinolone must be biologically active on a large spectrum of gram positiveand gram negative bacteria, aerobic and anaerobic germs and mycobacteria, must have as fewside effects as possible, excellent solubility in water and to be taken in orally.The goal of our reserch work was to obtaine by synthesis new quinolone derivatives withthe general formula:Figure 1R 6OCO 2 HR 7R 8NR 1R 1 = alkyl, p-nitro-phenyl, p-amino-phenyl;R 6 = hydrogen, fluor, chlor, methylR 7 = heterocycle;R 8 = hydrogen, chlor.The novel quinolones was evaluated for „in vitro” activity by determining minimum inhibitoryconcentration against a variety of bacteria. In conclusion, the results of the present paper indicate that substituentcombinations in the quinolone ring might produce powerful antibacterial agents.