Synthesis and biological evaluation of new fluconazole β-lactam conjugates linked via 1,2,3-triazoleElectronic supplementary information (ESI) available: Experimental details, proton and carbon NMR spectra of new compounds and tables of biological activity associated with this article can be found, in the online version, at http://dx.doi.org/10.1016/. See DOI: 10.1039/c6nj03117j
Novel 1,2,3-triazole-linked β-lactam-fluconazole conjugates 12(a-l) were designed and synthesized. The compounds showed potent antifungal activity against two pathogenic Candida strains; Candida albicans ATCC 24433 and Candida albicans ATCC 10231 with MIC values in the range of 0.0625-2 μg mL −1 . C...
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Sprache: | eng |
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Zusammenfassung: | Novel 1,2,3-triazole-linked β-lactam-fluconazole conjugates
12(a-l)
were designed and synthesized. The compounds showed potent antifungal activity against two pathogenic
Candida
strains;
Candida albicans
ATCC 24433 and
Candida albicans
ATCC 10231 with MIC values in the range of 0.0625-2 μg mL
−1
. Compounds
12h
,
12j
and
12k
showed promising antifungal activity against all the tested fungal pathogens except
C. neoformans
ATCC 34554 compared to fluconazole. Compound
12j
in which the β-lactam ring was formed using
para
-anisidine and benzaldehyde was found to be more potent than fluconazole against all the fungal strains with an IC
50
value of |
---|---|
ISSN: | 1144-0546 1369-9261 |
DOI: | 10.1039/c6nj03117j |