Synthesis of isothiochroman 2,2-dioxide and 1,2-benzooxathiin 2,2-dioxide gyrase B inhibitors
详细信息 查看全文
- 作者：Peixoto ; Christophe ; Laurin ; Patrick ; Klich ; Michel ; Dupuis-Hamelin ; Claudine ; Mauvais ; Pascale ; et. al.
- 关键词：antibiotics ; glycosidation ; hydrogen bonding ; structure&ndash ; activity
- 刊名：Tetrahedron Letters
- 出版年：2000
- 出版时间：March 11, 2000
- 年：2000
- 卷：41
- 期：11
- 页码：1741-1745
- 全文大小：168 K
文摘
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.