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Synthesis and antibacterial activity of 2α-functionalized 1β-methylcarbapenems related to KR-21012

✍ Scribed by Hyun J. Kwak; Do K. Pyun; Jae H. Kim; Eun J. Kim; Hee J. Jeong; Bong J. Kim; Cheol H. Lee


Publisher
Elsevier Science
Year
2000
Tongue
English
Weight
148 KB
Volume
10
Category
Article
ISSN
0960-894X

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✦ Synopsis


AbstractÐThe 2a-functionalized 1b-methylcarbapenems 3 were synthesized from the 2-formyl 1b-methylcarbapenem intermediate 5. The best compound in the series of 2a-(hydroxy)alkylcarbapenems, KR-21012, displayed well balanced in vitro and in vivo activity as a parent compound of oral carbapenem.


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The synthesis of a new series of 1 beta-methylcarbapenems having a 1,3-diazabicyclo[3.3.0]octane-2,4-dione moiety is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bateria are determined and the effect of substituent on the bicyclic ring as well as st