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

โœ Scribed by Christophe Peixoto; Patrick Laurin; Michel Klich; Claudine Dupuis-Hamelin; Pascale Mauvais; Patrice Lassaigne; Alain Bonnefoy; Branislav Musicki


Publisher
Elsevier Science
Year
2000
Tongue
French
Weight
168 KB
Volume
41
Category
Article
ISSN
0040-4039

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โœฆ Synopsis


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.


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