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  • Title: Novel imidazole substituted 6-methylidene-penems as broad-spectrum beta-lactamase inhibitors.
    Author: Venkatesan AM, Agarwal A, Abe T, Ushirogochi H, Yamamura I, Kumagai T, Petersen PJ, Weiss WJ, Lenoy E, Yang Y, Shlaes DM, Ryan JL, Mansour TS.
    Journal: Bioorg Med Chem; 2004 Nov 15; 12(22):5807-17. PubMed ID: 15498657.
    Abstract:
    Beta-lactamases are serine and metallo-dependent enzymes produced by the bacteria in defense against beta-lactam antibiotics. Production of class-A, class-B, and class-C enzymes by the bacteria make the use of beta-lactam antibiotics ineffective in certain cases. To overcome resistance to beta-lactam antibiotics, several beta-lactamase inhibitors such as clavulanic acid, sulbactam, and tazobactam are widely used in the clinic in combination with beta-lactam antibiotics. However, single point mutations within these enzymes have allowed bacteria to overcome the inhibitory effect of the commercially approved beta-lactamase inhibitors. Although the commercially available beta-lactamase inhibitor/beta-lactam antibiotic combinations are effective against class-A producing bacteria and many extended spectrum beta-lactamase (ESBL's) producing bacteria they are less effective against class-C enzymes expressing bacteria. To circumvent this problem, based on modeling studies several novel imidazole substituted 6-methylidene-penem derivatives were synthesized and tested against various beta-lactamase producing isolates. The present paper deals with the synthesis and structure-activity relationships (SAR) of these compounds.
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