The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
SEMISYNTHETIC CEPHALOSPORINS WITH ANTIFUNGAL ACTIVITY: LABORATORY STUDIES ON 2-PYRIDINETHIOL 1-OXIDE CEPHALOSPORINS
JOSEPH V. URIPAUL ACTORLILLIAN PHILLIPSJERRY A. WEISBACH
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JOURNAL FREE ACCESS

1978 Volume 31 Issue 6 Pages 580-585

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Abstract
Cephalosporins are chemotherapeutic agents whose spectrum and use are limited to antibacterial activity. Therefore, it was of interest to find several new semisynthetic cephalosporins which possess in vitro antifungal activity against Trichophyton mentagrophytes, Candida albicans and certain other yeasts. Five new cephalosporins containing the 2-pyridinethiol 1- oxide grouping were examined. Four with this heterocyclic moiety in the 3-position were found to have activity. One with the grouping in the 7-acyl-side chain was inactive. The degree of the antifungal activity was influenced by the substituent at the 7-position. The cephalosporin with a p-hydroxyphenylglycyl side chain was the most potent against the fungal strains studied. Despite this in vitro antifungal activity, none of the compounds protected mice against a systemic Candida albicans infection. All of these cephalosporins had broad spectrum in vitro and in vivo antibacterial activity.
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© Japan Antibiotics Research Association
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