Bazı yeni fluorokinolon türevlerinin sentezi ve biyolojik etkilerinin incelenmesi

Abstract

Literatürde kayıtlı kloroasetamit türevlerinin uygun tepkime şartlarındasiprofloksazin veya norfloksazin ile tepkimesi sonucunda hedeflenen 7-[4-(2-{[4-(sübstitüefenil/ adamantil)-1,3-tiyazol-2-il]amino}-2-oksoetil)piperazin-1-il]-1-etil/ siklopropil-6-fluoro-4-okso-1,4-dihidrokinolin-3-karboksilik asit ve 7-[4-(2-{[5-(nonsübstitüe/ alkil/ sülfamoil)-1,3,4-tiyadiazol-2-il]amino}-2-oksoetil)piperazin-1-il]-1-etil/ siklopropil-6-fluoro-4-okso-1,4-dihidrokinolin-3-karboksilik asit türevleri sentezlenmiştir. Sentezlenen bileşiklerin antibakteriyel aktivitesi mikrodilüsyon yöntemi iledeğerlendirilmiştir. 7- [4- (2 - {[1,3,4-tiyadiazol-2-il] amino} -2-oksoetil) piperazin-1-il] -1-siklopropil-6-fluoro-4-okso-1, 4-dihidrokinolin-3-karboksilik asit (3g), Escherichia coliATCC 25922, Yersinia pseudotuberculosis ATCC 911, Klebsiella pneumonia vePseudomonas aeruginosa ATCC 43288 suşlarına karşı <0.63 μg/ ml MİK değeriyle aktifolarak bulunmuştur.

Novel 7-[4-(2-{[4-(Substituted phenyl / adamantyl)-1,3-thiazole-2-yl]amino}-2-oxoethyl)piperazin-1-yl]-1-ethyl/ cyclopropyl-6-floro-4-oxo-1,4-dihidroquinoline-3-carboxylic acid and 7-[4-(2-{[5-(nonsubstituted/ alkyl/ sulfamoyl)-1,3,4-thiadiazole-2-yl]amino}-2-oxoethyl)piperazin-1-yl]-1-ethyl/ cyclopropyl-6-floro-4-oxo-1,4-dihidroquinoline-3-carboxylic acid derivatives were synthesized by the reaction ofnorfloxacin or ciprofloxacin with chloroacetamide derivatives which have already beenreported in literature. Antibacterial activity of synthesized compounds was evaluated by usingmicrodilution method. 7-[4-(2-{[1,3,4-thiadiazole-2-yl]amino}-2-oxoethyl)piperazine-1-yl]-1-cyclopropyl -6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (3g) was found to beactive against Escherichia coli ATCC 25922, Yersinia pseudotuberculosis ATCC 911,Klebsiella pneumonia and Pseudomonas aeruginosa ATCC 43288 with the MIC values of<0.63 μg/ ml.