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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Hauptverfasser: Divse, Jaisingh M, Mhaske, Santosh B, Charolkar, Chaitanya R, Sant, Duhita G, Tupe, Santosh G, Deshpande, Mukund V, Khedkar, Vijay M, Nawale, Laxman U, Sarkar, Dhiman, Pore, Vandana S
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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