Synthesis and Antibacterial Activity of 1β‐Methyl‐2‐[5‐(1,2‐Disubstituted Ethyl)Pyrrolidin‐3‐ylthio]Carbapenem Derivatives

Abstract

The synthesis of a new series of 1beta-methylcarbapenems having a 5-(1,2-disubstituted ethyl) pyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of the substituent on the pyrrolidine ring was investigated. A particular compound IIIf having a 1-methoxyimino-2-carbamoylethyl substituted moiety showed the most potent antibacterial activity.

Biological evaluation of novel 1,4-dithiine derivatives as potential antimicrobial agents

“…Recently, derivatives of other heterocycle, 1,4-dithiine, were found as the new class of antimicrobial agents with activity against broad spectrum of Gram-positive and Gram-negative pathogens and fungal strains (Zentz et al, 2005). Sulphur atom could be also incorporated in nonaromatic part of the drug molecule, forming sulfanyl (Nawrozkij et al, 2008) or thiol (Hadizadeh and Mehrparvar, 2004;Ahn et al, 2006) groups. There is an increasing concern on thioureas as some of them also have been reported as antiviral agents, e.g.…”