Document Report Card
Basic Information
ID: ALA1132054
Journal: Bioorg Med Chem Lett
Title: Synthesis and properties of 2-(naphthosultamyl)methyl-carbapenems with potent anti-MRSA activity: discovery of L-786,392.
Authors: Ratcliffe RW, Wilkening RR, Wildonger KJ, Waddell ST, Santorelli GM, Parker DL, Morgan JD, Blizzard TA, Hammond ML, Heck JV, Huber J, Kohler J, Dorso KL, St Rose E, Sundelof JG, May WJ, Hammond GG.
Abstract: A series of 1beta-methyl-2-(naphthosultamyl)methyl-carbapenems bearing dicationic groups on the naphthosultamyl moiety was prepared and evaluated for activity against resistant gram-positive bacteria. Based on a combination of excellent in vitro antibacterial activity, acceptable mouse acute toxicity, and a desirable fragmentation pattern on beta-lactam ring opening, the analog 2g (L-786,392) was selected for extended evaluation.
CiteXplore: 10201828