Synthesis of Isothiochroman 2,2‐Dioxide and 1,2‐Benzooxathiin 2,2‐Dioxide Gyrase B Inhibitors.

Abstract The design, synthesis and in vitro biological evaluation of isothiochroman 2,2-dioxide and 1,2-benzooxathiin 2,2-dioxide analogues of coumarin inhibitors of gyrase B are described. Compared to coumarin derivatives, compounds of the 1,2-benzooxathiin 2,2-dioxide series display improved inhibitory potency in negative supercoiling of relaxed DNA gyrase.