Structure--activity relationship of quinolones.
The understanding of some structure-activity relationships of quinolones allowed the development of the new fluorinated quinolones, compounds with a major clinical potential. The basic structure of these drugs consists of a substituted pyridine ring and a carboxylic acid ring. The substitution at the first position is vital for antibacterial activity, while the presence of a fluorine atom and a piperazine ring is responsible for a broader spectrum of activity and higher intrinsic potency. Further modifications at side-chains or on the ring structure provide compounds with different pharmacokinetic or/and antibacterial activity. A better understanding of these relationships and correlations with clinical results is essential for the design of new improved derivatives with therapeutic potential.
Toma
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Division of Microbiology, Hôtel-Dieu de Montréal, Québec.
D055598:Chemical Phenomena; D002621:Chemistry; D015195:Drug Design; D015363:Quinolones; D013329:Structure-Activity Relationship
D015363:Quinolones