Synthesis and antibacterial activity of C-2 carboxyethenylthio-carbapenem derivatives.
A number of C-2 carboxyethenylthio-carbapenem derivatives possessing either the (5R,6R,8S)- or the (5R,6S,8R)-stereochemistries have been prepared from the olivanic acids MM 22382 (1) and MM 22383 (4), respectively. Their in vitro antibacterial activities and stabilities to human kidney homogenate are superior to those of the parent compounds, particularly in the latter series.
Beecham Pharmaceuticals, Research Division, Brockham Park, Betchworth, Surrey, UK.
M J
MJ
Basker
D F
DF
Corbett
S
S
Coulton
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R
Southgate
D000818:Animals; D001419:Bacteria / Q000187:drug effects*; D015780:Carbapenems / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D055598:Chemical Phenomena; D002621:Chemistry; D046508:Culture Techniques; D004355:Drug Stability; D004927:Escherichia coli Infections / Q000188:drug therapy; D006801:Humans; D007668:Kidney / Q000378:metabolism; D051379:Mice; D008968:Molecular Conformation; D015394:Molecular Structure; D013203:Staphylococcal Infections / Q000188:drug therapy; D013237:Stereoisomerism
D015780:Carbapenems