Azide-enolate 1,3-dipolar cycloaddition in the synthesis of novel triazole-based miconazole analogues as promising antifungal agents

作者：Gonzalez Calderon Davir; Mejia Dionicio Maria G; Morales Reza Marco A; Ramirez Villalva Alejandra; Morales Rodriguez Macario; Jauregui Rodriguez Bertha; Diaz Torres Eduardo; Gonzalez Romero Carlos; Fuentes Benites Aydee

来源：European Journal of Medicinal Chemistry, 2016, 112: 60-65.

DOI：10.1016/j.ejmech.2016.02.013

• Miconazole analogs
• 1,2,3-Triazole derivatives
• Antifungal activity
• Azide-enolate cycloaddition

Seven miconazole analogs involving 1,4,5-tri and 1,5-disubstituted triazole moieties were synthesized by azide-enolate 1,3-dipolar cycloaddition. The antifungal activity of these compounds was evaluated in vitro against four filamentous fungi, including Aspergillus fumigatus, Trichosporon cutaneum, Rhizopus oryzae, and Mucor hiemalis as well as three species of Candida spp. as yeast specimens. These pre-clinical studies suggest that compounds 4b, 4d and 7b can be considered as drug candidates for future complementary biological studies due to their good/excellent antifungal activities.

• 出版日期2016-4-13