Affiliation:
1. Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, Minia 61519, Egypt
Abstract
Fluoroquinolones represent an interesting synthetic class of antimicrobial agents with broad spectrum and potent activity. Since the discovery of nalidixic acid, the prototype of quinolones, several structural modifications to the quinolone nucleus have been carried out for improvement of potency, spectrum of activity, and to understand their structure activity relationship (SAR). The C-7 substituent was reported to have a major impact on the activity. Accordingly, Substitution at C-7 or its N-4-piperazinyl moiety was found to affect potency, bioavailability, and physicochemical properties. Also, it can increase the affinity towards mammalian topoisomerases that may shift quinolones from antibacterial to anticancer candidates. Moreover, the presence of DNA topoisomerases in both eukaryotic and prokaryotic cells makes them excellent targets for chemotherapeutic intervention in antibacterial and anticancer therapies. Based on this concept, several fluoroquionolones derivatives have been synthesized and biologically evaluated as antibacterial, antituberculosis, antiproliferative, antiviral and antifungal agents. This review is an attempt to focus on the therapeutic prospects of fluoroquinolones with an updated account on their atypical applications such as antitubercular and anticancer activities.
Publisher
Bentham Science Publishers Ltd.
Subject
Pharmacology,Molecular Medicine,Drug Discovery,Biochemistry,Organic Chemistry
Reference162 articles.
1. Sharma P.C.; Jain A.; Jain S.; Fluoroquinolone antibacterials: a review on chemistry, microbiology and therapeutic prospects. Acta Pol Pharm 2009,66(6),587-604
2. Hooper D.C.; Clinical applications of quinolones. Biochim Biophys Acta 1998,1400(1-3),45-61
3. Bisacchi G.S.; Origins of the quinolone class of antibacterials: an expanded “Discovery Story”. J Med Chem 2015,58(12),4874-4882
4. Davies J.; Davies D.; Origins and evolution of antibiotic resistance. Microbiol Mol Biol Rev 2010,74(3),417-433
5. Slater A.F.; Cerami A.; Inhibition by chloroquine of a novel haem polymerase enzyme activity in malaria trophozoites. Nature 1992,355(6356),167-169
Cited by
40 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献