Synthesis of isothiochroman 2, 2-dioxide and 1, 2-benzooxathiin 2, 2-dioxide gyrase B inhibitors

…, M Klich, C Dupuis-Hamelin, P Mauvais, P Lassaigne…

Index: Peixoto, Christophe; Laurin, Patrick; Klich, Michel; Dupuis-Hamelin, Claudine; Mauvais, Pascale; Lassaigne, Patrice; Bonnefoy, Alain; Musicki, Branislav Tetrahedron Letters, 2000 , vol. 41, # 11 p. 1741 - 1745

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Citation Number: 23

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.