Pyrazolo[4,3-c][1,2]benzothiazines 5,5-Dioxide: A Promising New Class of Staphylococcus aureus NorA Efflux Pump Inhibitors

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• 作者：Stefano Sabatini ; Francesca Gosetto ; Serena Serritella ; Giuseppe Manfroni ; Oriana Tabarrini ; Nunzio Iraci ; Jean Pierre Brincat ; Emanuele Carosati ; Milena Villarini ; Glenn W. Kaatz ; Violetta Cecchetti
• 刊名：Journal of Medicinal Chemistry
• 出版年：2012
• 出版时间：April 12, 2012
• 年：2012
• 卷：55
• 期：7
• 页码：3568-3572
• 全文大小：270K
• 年卷期：v.55,no.7(April 12, 2012)
• ISSN：1520-4804

文摘

The increasing resistance to antibacterials commonly employed in the clinic and the growth of multidrug resistant strains suggest that the development of new therapeutic approaches should be of primary concern. In this context, EPIs may restore life to old drugs. In the present work, the EPI activity of the COX-2 inhibitor celecoxib was confirmed and a new class of pyrazolo[4,3-c][1,2]benzothiazine 5,5-dioxide analogues acting as inhibitors of the Staphylococcus aureus NorA multidrug efflux pump was identified.