The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Synthesis and Structure-activity Relationships of a Novel Oral Carbapenem, CS-834
MASAO MIYAUCHIROKURO ENDOMASAFUMI HISAOKAHIROSHI YASUDAISAO KAWAMOTO
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1997 年 50 巻 5 号 p. 429-439

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We have studied an ester prodrug of a carbapenem to develop a potent orally active β-lactam antibiotic. A variety of 1β-methylcarbapenem derivatives have been synthesized. We have found that some derivatives having an amide group in the C-2 side chain show potent and well balanced antibacterial activities as well as high stability against dehydropeptidase-I. Oral absorption of derivatives has been optimized by modifying the C-3 ester promoiety. Pivaloyloxymethyl (1R, 5S, 6S)-6-[(R)-1-hydroxyethyl]-1-methyl-2-[(R)-5-oxopyrrolidin-3-ylthio]-1-carbapen-2-em-3-carboxylate, CS-834, has been selected as the most promising compound for further evaluation.

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