Synthesis and in vitro antibacterial activity of new meropenem analogs

Title
Synthesis and in vitro antibacterial activity of new meropenem analogs
Authors
엘가말김성종오창현
Keywords
antibacterial activity; imipenem; meropenem; methoxyimino
Issue Date
2011-10
Publisher
Journal of antibiotics
Citation
VOL 64, NO 10, 687-688
Abstract
Carbapenems are one of the most potent types of antibacterial agents and are among those used as a last resort against infections in the clinical field. Recently, they have been classified into three classes according to their chemical structures. According to this classification, meropenem belongs to 1β-methylcarbapenems containing (3S)- pyrrolidine-3-ylthio moiety.1 The 1β-methyl group slows renal hydrolysis by dehydropeptidase-I (DHP-I) and allows usage as a single agent.2,3 Carbapenems with (3S)-pyrrolidine-3-ylthio moiety are reported for their broad-spectrum and potent antibacterial activity.4 In the present investigation, we report the synthesis and in vitro antibacterial evaluation of three new meropenem analogs against 18 bacterial strains. Our target is to discover new carbapenem derivatives with improved antibacterial activity (Figure 1). Our general synthetic route leading to new carbapenem derivatives involved the preparation of appropriately protected thiols containing pyrrolidine ring as a side chain and coupling reaction with the carbapenem diphenylphosphate, followed by deprotection of the resulting protected carbapenems in a usual manner.
URI
http://pubs.kist.re.kr/handle/201004/40791
ISSN
0021-8820
Appears in Collections:
KIST Publication > Article
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