Novel inhibitors of Erm methyltransferases from NMR and parallel synthesis

…, JM Schkeryantz, D Janowick, M Kaminski…

文献索引：Hajduk, Philip J.; Dinges, Juergen; Schkeryantz, Jeffrey M.; Janowick, David; Kaminski, Michele; Tufano, Michael; Augeri, David J.; Petros, Andrew; Nienaber, Vicki; Zhong, Ping; Hammond, Rachel; Coen, Michael; Beutel, Bruce; Katz, Leonard; Fesik, Stephen W. Journal of Medicinal Chemistry, 1999 , vol. 42, # 19 p. 3852 - 3859

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被引用次数: 117

摘要

The Erm family of methyltransferases confers resistance to the macrolide-lincosamide- streptogramin type B (MLS) antibiotics through the methylation of 23S ribosomal RNA. Upon the methylation of RNA, the MLS antibiotics lose their ability to bind to the ribosome and exhibit their antibiotic activity. Using an NMR-based screen, we identified a series of triazine- containing compounds that bind weakly to ErmAM. These initial lead compounds were ...