title: Pyrazolo[4,3-c][1,2]benzothiazines 5,5-dioxide: a promising new class of Staphylococcus aureus NorA efflux pump inhibitors.
abstract: 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.
authors.affiliation: Dipartimento di Chimica e Tecnologia del Farmaco,Università degli Studi di Perugia, 06123 Perugia, Italy. stefano.sabatini@unipg.it
authors.forename: Stefano
authors.initials: S
authors.lastname: Sabatini
authors.forename: Francesca
authors.initials: F
authors.lastname: Gosetto
authors.forename: Serena
authors.initials: S
authors.lastname: Serritella
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Manfroni
authors.forename: Oriana
authors.initials: O
authors.lastname: Tabarrini
authors.forename: Nunzio
authors.initials: N
authors.lastname: Iraci
authors.forename: Jean Pierre
authors.initials: JP
authors.lastname: Brincat
authors.forename: Emanuele
authors.initials: E
authors.lastname: Carosati
authors.forename: Milena
authors.initials: M
authors.lastname: Villarini
authors.forename: Glenn W
authors.initials: GW
authors.lastname: Kaatz
authors.forename: Violetta
authors.initials: V
authors.lastname: Cecchetti
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors*; D000068579:Celecoxib; D052246:Cyclooxygenase 2 Inhibitors / Q000737:chemistry / Q000494:pharmacology; D024901:Drug Resistance, Multiple, Bacterial; D004357:Drug Synergism; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D027425:ATP-Binding Cassette, Sub-Family C Proteins / Q000037:antagonists & inhibitors*; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D054852:Small Molecule Libraries; D013211:Staphylococcus aureus / Q000187:drug effects / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology; D013843:Thiazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; D000068579:Celecoxib; D052246:Cyclooxygenase 2 Inhibitors; D027425:ATP-Binding Cassette, Sub-Family C Proteins; D011720:Pyrazoles; D054852:Small Molecule Libraries; D013449:Sulfonamides; D013843:Thiazines; C075040:NorA protein, Staphylococcus