In:
Chemotherapy, S. Karger AG, Vol. 47, No. 3 ( 2001), p. 170-176
Abstract:
We evaluated a series of novel cephem antibiotics, N-alkylpyridinium (alkyl group), N-carboxyethylpyridinium (carboxylic group), N-sulfoethylpyridinium (sulfonic group) and N-alkylquaternary ammonium salts (ammonioethyl group), N-alkyl-aromatic-quaternary ammonium salts and N-alkyl-heterocyclic quaternary ammonium salts (cyclic group) as vinylthio pyridinium derivatives at the C-3 position and hydroxyiminoaminothiazol at the C-7 position, for their activity against methicillin-resistant 〈 i 〉 Staphylococcus aureus 〈 /i 〉 (MRSA) and their solubility, by measuring the minimum inhibitory concentrations (MICs) and the dissolving test in phosphate buffer. All tested compounds, except for the alkyl group, showed good solubility ( 〉 10%) in 1/15 〈 i 〉 M 〈 /i 〉 phosphate buffer (pH 7.2). The concentrations required to inhibit 80% of the bacterial strains (MIC 〈 sub 〉 80 〈 /sub 〉 s) of the alkyl group, carboxylic group, sulfonic group, ammonioethyl group and cyclic group against MRSA were 1.56, 12.5–25, 6.25, 1.56 and 1.56 µg/ml, respectively. These results indicated that the ammonioethyl and cyclic groups yield the maximum anti-MRSA and anti- 〈 i 〉 Enterococcus 〈 /i 〉 〈 i 〉 faecalis 〈 /i 〉 activity, and also good water solubility.
Type of Medium:
Online Resource
ISSN:
0009-3157
,
1421-9794
Language:
English
Publisher:
S. Karger AG
Publication Date:
2001
detail.hit.zdb_id:
1482111-4
SSG:
15,3
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