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

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

Bioorganic & medicinal chemistry letters (1999-04-14)

R R Wilkening, R W Ratcliffe, K J Wildonger, L D Cama, K D Dykstra, F P DiNinno, T A Blizzard, M L Hammond, J V Heck, K L Dorso, E St Rose, J Kohler, G G Hammond

PMID10201827

摘要

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.