The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
STUDIES ON β-LACTAM ANTIBIOTICS. VII
EFFECT ON ANTIBACTERIAL ACTIVITY OF THE OXIME O-SUBSTITUENTS WITH VARIOUS FUNCTIONAL GROUPS IN THE 7β-[(Z)-2-(2-AMINO- 4-THIAZOLYL)-2-OXYIMINOACETAMIDO]CEPHALOSPORINS
HISASHI TAKASUGIHIROMU KOCHITAKASHI MASUGIHIROSHI NAKANOTAKAO TAKAYA
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1983 Volume 36 Issue 7 Pages 846-854

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Abstract

The synthesis and in vitro activity of the 7-[O-substituted oxyiminoacetamido]cephalosporins (I) without substitution at 3-position of a cephem nucleus are described. Effect of changing the oxime O-substituents (R1) with various functional groups in the 7-acyl residue on antibacterial activity was examined. Against Gram-positive bacteria, cephems with hydrophilic functions in the R1 moiety such as hydroxyethyl, aminoethyl and carboxymethyl groups showed decrease of the activity, while cephems with lipophilic functions such as cyanomethyl, methylthiomethyl and halogenoethyl groups exhibited increase of the activity. However, influence of the substituents (R1) on activity against Gram-negative bacteria was observed to be relatively independent of the nature of their functional groups.

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