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ID: ALA1132053

Journal: Bioorg Med Chem Lett

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

Authors: Wilkening RR, Ratcliffe RW, Wildonger KJ, Cama LD, Dykstra KD, DiNinno FP, Blizzard TA, Hammond ML, Heck JV, Dorso KL, St Rose E, Kohler J, Hammond GG.

Abstract: A series of 1beta-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.

CiteXplore: 10201827

DOI: 10.1016/s0960-894x(99)00070-0