혼성 Bivalent Ligand 퀴놀론 유도체의 합성

Synthesis of Hybrid Bivalent Ligand Quinolone Derivatives

Eighteen new hybrid bivalent ligand quinolones that contain two different type of pharmacophores in a single molecule were prepared and evaluated for in vitro antibacterial activity. Hybrid bivalent ligands p-nitrobenzyloxycarbonyl quinolones were prepared by the treatment of active esters of succinyl fluoroquinolones with 1,7-disubstituted fluoroquinolone carboxylic acids in DMF. Eighteen final quinolone carboxylic acids were obtained by the reduction of compounds 25~42 with hydrogen in the presence of 1001o Pd-C. Among these derivatives, compound[56] showed the most potent antibacterial activity against a wide range of microoranisms.