Structure-based design, synthesis, and antimicrobial activity of indazole-derived SAH/MTA nucleosidase inhibitors

…, M Khalili, Z Nie, S Margosiak, V Nikulin…

文献索引：Li, Xiaoming; Chu, Sam; Feher, Victoria A.; Khalili, Mitra; Nie, Zhe; Margosiak, Stephen; Nikulin, Victor; Levin, James; Sprankle, Kelly G.; Tedder, Martina E.; Almassy, Robert; Appelt, Krzysztof; Yager, Kraig M. Journal of Medicinal Chemistry, 2003 , vol. 46, # 26 p. 5663 - 5673

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被引用次数: 85

摘要

The structure-based design, synthesis, and biological activity of a novel indazole-containing inhibitor series for S-adenosyl homocysteine/methylthioadenosine (SAH/MTA) nucleosidase are described. Use of 5-aminoindazole as the core scaffold provided a structure-guided series of low nanomolar inhibitors with broad-spectrum antimicrobial activity. The implementation of structure-based methodologies provided a 6000-fold increase in ...