期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 7, 期 4, 页码 374-378出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.5b00368
关键词
Antibacterials; DNA gyrase B; fragment-based drug design; structure-based drug design
The ATPase subunit of DNA gyrase B is an attractive antibacterial target due to high conservation across bacteria and the essential role it plays in DNA replication. A novel class of pyrazolopyridone inhibitors was discovered by optimizing a fragment screening hit scaffold using structure guided design. These inhibitors show potent Gram-positive antibacterial activity and low resistance incidence against clinically important pathogens.
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