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ID: ALA1130748
Journal: Bioorg Med Chem Lett
Title: Design and synthesis of monocyclic beta-lactams as mechanism-based inhibitors of human cytomegalovirus protease.
Authors: Borthwick AD, Weingarten G, Haley TM, Tomaszewski M, Wang W, Hu Z, Bedard J, Jin H, Yuen L, Mansour TS.
Abstract: Mechanism based inhibitors of HCMV protease have been designed based on the monocyclic beta-lactam nucleus, which have been shown to acylate the viral enzyme in a time dependent manner. SAR in a series of monocyclic beta-lactam N-ureas, has defined the size and relative stereochemistry of the C-3 substituent producing a low micromolar inhibitor 17b with good aqueous stability and selectivity over the mammalian serine proteases.
CiteXplore: 9871686