Synthesis and properties of 2-(naphthosultamyl)methylcarbapenems 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
Citation
Rw. Ratcliffe et al., Synthesis and properties of 2-(naphthosultamyl)methylcarbapenems with potent anti-MRSA activity: Discovery of L-786,392, BIOORG MED, 9(5), 1999, pp. 679-684
Citations number
21
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
5
Year of publication
1999
Pages
679 - 684
Database
ISI
SICI code
0960-894X(19990308)9:5<679:SAPO2W>2.0.ZU;2-L
Abstract
A series of 1 beta-methyl-2-(naphthosultamyl)methyl-carbapenems bearing dic ationic 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 toxici ty, and a desirable fragmentation pattern on beta-lactam ring opening, the analog 2g (L-786,392) was selected for extended evaluation. (C) 1999 Elsevi er Science Ltd. All rights reserved.