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

被引:43
作者
Ouahrouch, Abdelaaziz [1 ,2 ,3 ]
Ighachane, Hana [2 ,4 ]
Taourirte, Moha [1 ]
Engels, Joachim W. [3 ]
Sedra, My Hassan [4 ]
Lazrek, Hassan B. [2 ]
机构
[1] FSTG, Dept Chem, Lab Bioorgan & Macromol Chem, Marrakech, Morocco
[2] Fac Sci Semlalia, Dept Chem, Lab Biomol & Med Chem, Marrakech, Morocco
[3] Goethe Univ Frankfurt, Inst Organ Chem & Chem Biol, D-60438 Frankfurt, Germany
[4] INRA, Lab Genet Phytopathol & Microbial Control, Marrakech, Morocco
关键词
Antibacterial activity; Antifungal activity; Hybrid molecules; TOPOISOMERASE-II; INTERCALATION COMPLEXES; DNA-INTERCALATION; MITOXANTRONE; ANTITUMOR; AMSACRINE; DESIGN; DRUGS;
D O I
10.1002/ardp.201400142
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:748 / 755
页数:8
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