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Pyrazolo[4,3-c][1,2]benzothiazines 5,5-Dioxide: A Promising New Class of Staphylococcus aureus NorA Efflux Pump Inhibitors
dataset
posted on 2012-04-12, 00:00 authored by Stefano Sabatini, Francesca Gosetto, Serena Serritella, Giuseppe Manfroni, Oriana Tabarrini, Nunzio Iraci, Jean Pierre Brincat, Emanuele Carosati, Milena Villarini, Glenn
W. Kaatz, Violetta CecchettiThe 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.