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  • Title: Synthesis and activity of 2-(sulfonamido)methyl-carbapenems: discovery of a novel, anti-MRSA 1,8-naphthosultam pharmacophore.
    Author: 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.
    Journal: Bioorg Med Chem Lett; 1999 Mar 08; 9(5):673-8. PubMed ID: 10201827.
    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.
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