Novel pyrazole derivatives as potent inhibitors of type II topoisomerases. Part 1: synthesis and preliminary SAR analysis

…, J Wu, JJM Wiener, H Venkatesan, A Santillán…

文献索引：Gomez, Laurent; Hack, Michael D.; Wu, Jiejun; Wiener, John J.M.; Venkatesan, Hari; Santillan Jr., Alejandro; Pippel, Daniel J.; Mani, Neelakandha; Morrow, Brian J.; Motley, S. Timothy; Shaw, Karen Joy; Wolin, Ronald; Grice, Cheryl A.; Jones, Todd K. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 10 p. 2723 - 2727

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被引用次数: 65

摘要

In an attempt to search for a new class of antibacterial agents, we have discovered a series of pyrazole analogs that possess good antibacterial activity for Gram-positive and Gram- negative organisms via inhibition of type II bacterial topoisomerases. We have investigated the structure–activity relationships of this series, with an emphasis on the length and conformation of the linker. This work led to the identification of tetrahydroindazole analogs, ...