Synthesis and activity of 2-(sulfonamido) methyl-carbapenems: Discovery of a novel, anti-MRSA 1, 8-naphthosultam pharmacophore

…, LD Cama, KD Dykstra, FP DiNinno, TA Blizzard…

文献索引：Wilkening; Ratcliffe; Wildonger; Cama; Dykstra; DiNinno; Blizzard; Hammond; Heck; Dorso; St Rose; Kohler Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 5 p. 673 - 678

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被引用次数: 28

摘要

A series of 1β-methyl carbapenems substituted at the 2-position with lipophilic, acyclic and cyclic (sulfonamido) methyl groups was prepared and evaluated for activity against resistant gram-positive bacteria. From these studies, the 1, 8-naphthosultamyl group emerged as a novel, PBP2a-binding, anti-MRSA pharmacophore worthy of further exploration.