The design, synthesis and in vitro biological evaluation of isothiochroman
2,2-dioxide and 1,2-benzooxathiin 2,2-dioxide analogues of coumarin inhibit
ors of gyrase B are described. Compared to coumarin derivatives, compounds
of the 1,2-benzooxathiin 2,2-dioxide series display improved inhibitory pot
ency in negative supercoiling of relaxed DNA gyrase. (C) 2000 Elsevier Scie
nce Ltd. All rights reserved.