4.5 Article

Benzimidazole-1,2,3-triazole Hybrid Molecules: Synthesis and Evaluation for Antibacterial/Antifungal Activity

Journal

ARCHIV DER PHARMAZIE
Volume 347, Issue 10, Pages 748-755

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201400142

Keywords

Antibacterial activity; Antifungal activity; Hybrid molecules

Funding

  1. Centre National de Recherche Scientifique et Technique (CNRST, Rabat, Morocco) [RS 2011/01]

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A novel series of hybrid molecules 4a-i and 5a-i were prepared by condensation of 4-(trimethylsilylethynyl)benzaldehyde 1 with substituted o-phenylenediamines. These in turn were reacted with 2-(azidomethoxy) ethyl acetate in a Cu alkyne-azide cycloaddition (CuAAC) to generate the 1,2,3-triazole pharmacophore under microwave assistance. The newly synthesized compounds were examined for their in vitro antimicrobial activities against Gram-positive and Gram-negative bacteria and the phytopathogenic fungi Verticillium dahliae and Fusarium oxysporum f. sp. albedinis. 2-((4-(4-(5-Trifluoromethyl benzimidazol-2-yl)phenyl)-1,2,3-triazol-1-yl)methoxy)ethanol 5e showed a moderate inhibition of 30% in the Foa sporulation test.

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