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Synthesis and Antifungal Activity Evaluation of 1-(2-Benzyloxy-2-Phenylethyl)-1,2,3-Triazole Miconazole Analogs
Pharmaceutical Chemistry Journal ( IF 0.8 ) Pub Date : 2021-08-14 , DOI: 10.1007/s11094-021-02440-x
Juana Suárez-García 1, 2 , Ma-Angeles Cano-Herrera 1, 2 , Nieves Zavala-Segovia 1, 3 , Marco A. García-Eleno 1, 2 , M. V. Basavanag Unnamatla 1, 2 , Erick Cuevas-Yañez 1, 2 , Alejandra Ramírez-Villalva 2 , Aydeé Fuentes-Benites 2
Affiliation  

Aseries of 1-(2-aryloxy-2-phenylethyl)-1,2,3-triazole derivatives (Miconazole analogs) was obtained via copper catalyzed azide-alkyne cycloaddition as the key step. The synthesized compounds were evaluated for antimicrobial activity against Candida genus strains as well as filamentous fungi (Mucor hiemalis, Aspergillus fumigatus and Rhizopus oryzae). A 1-(2-aryloxy-2-phenylethyl)-1,2,3-triazole derivative exhibited remarkable selectivity comparable to that of Itraconazole against Rhizopus oryzae.



中文翻译:

1-(2-苄氧基-2-苯基乙基)-1,2,3-三唑咪康唑类似物的合成和抗真菌活性评价

作为关键步骤,通过铜催化的叠氮化物-炔烃环加成反应获得了一系列 1-(2-芳氧基-2-苯乙基)-1,2,3-三唑衍生物(咪康唑类似物)。评价合成的化合物对念珠菌属菌株以及丝状真菌(Mucor hiemalisAspergillus fumigatusRhizopus oryzae)的抗菌活性。1-(2-芳氧基-2-苯乙基)-1,2,3-三唑衍生物对米根霉表现出与伊曲康唑相当的选择性。

更新日期:2021-08-19
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