Literature DB >> 10201828

Synthesis and properties of 2-(naphthosultamyl)methyl-carbapenems with potent anti-MRSA activity: discovery of L-786,392.

R W Ratcliffe1, R R Wilkening, K J Wildonger, S T Waddell, G M Santorelli, D L Parker, J D Morgan, T A Blizzard, M L Hammond, J V Heck, J Huber, J Kohler, K L Dorso, E St Rose, J G Sundelof, W J May, G G Hammond.   

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.

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Year:  1999        PMID: 10201828     DOI: 10.1016/s0960-894x(99)00071-2

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  In vitro and in vivo activities of novel 2-(thiazol-2-ylthio)-1beta-methylcarbapenems with potent activities against multiresistant gram-positive bacteria.

Authors:  Yutaka Ueda; Makoto Sunagawa
Journal:  Antimicrob Agents Chemother       Date:  2003-08       Impact factor: 5.191

  1 in total

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