Azole derivatives of 1,4-benzothiazine as antifungal agents.
A series of azole derivatives of 1,4-benzothiazine 7-14 was synthesized and evaluated for the in vitro and in vivo activity against Candida albicans. Secondary alcohol 10 and its ether derivative 13 showed very good efficacy against systemic candidiasis in a murine experimental model.
Fringuelli
R
R
Istituto di Chimica e Tecnologia del Farmaco, Università di Perugia, Italy.
Schiaffella
F
F
Bistoni
F
F
Pitzurra
L
L
Vecchiarelli
A
A
D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001393:Azoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects*; D002177:Candidiasis / Q000188:drug therapy* / Q000401:mortality; D004195:Disease Models, Animal; D005260:Female; D051379:Mice; D008826:Microbial Sensitivity Tests; D013047:Specific Pathogen-Free Organisms; D013329:Structure-Activity Relationship; D013843:Thiazines / Q000138:chemical synthesis*
D000935:Antifungal Agents; D001393:Azoles; D013843:Thiazines