Structure-activity relationship of 6-methylidene penems bearing 6, 5 bicyclic heterocycles as broad-spectrum β-lactamase inhibitors: evidence for 1, 4-thiazepine …

…, M Ado, T Tsuyoshi, O Dos Santos, Y Gu…

文献索引：Venkatesan, Aranapakam M.; Agarwal, Atul; Abe, Takao; Ushirogochi, Hideki; Yamamura, Itsuka; Ado, Mihira; Tsuyoshi, Takasaki; Dos Santos, Osvaldo; Gu, Yansong; Sum, Fuk-Wah; Li, Zhong; Francisco, Gerry; Lin, Yang-I.; Petersen, Peter J.; Yang, Youjun; Kumagai, Toshio; Weiss, William J.; Shlaes, David M.; Knox, James R.; Mansour, Tarek S. Journal of Medicinal Chemistry, 2006 , vol. 49, # 15 p. 4623 - 4637

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被引用次数: 42

摘要

The design and synthesis of a series of 6-methylidene penems containing [6, 5]-fused bicycles (thiophene, imidazole, or pyrazle-fused system) as novel class A, B, and C β- lactamase inhibitors is described. These penems proved to be potent inhibitors of the TEM-1 (class A) and AmpC (class C) β-lactamases and less so against the class B metallo-β- lactamase CcrA. Their in vitro and in vivo activities in combination with piperacillin are ...