Molecular Sciences Institute, School of Chemistry, University of the Witwatersrand, PO Wits 2050, Johannesburg, South Africa.
Org Biomol Chem. 2014 Jan 14;12(2):307-15. doi: 10.1039/c3ob41798k.
The synthesis of 7-azaindoles from 3-alkynyl-2-aminopyridines using acidic conditions, namely, a mixture of trifluoroacetic acid (TFA) and trifluoroacetic anhydride (TFAA), is described. This methodology resulted in the synthesis of fifteen 7-azaindoles, with most containing substituents at the 2- and 5-positions. The majority of these were tested for antimicrobial activity against a range of bacteria and yeasts. The 7-azaindoles displayed the best activity against the yeasts, particularly against Cryptococcus neoformans, where activities as low as 3.9 μg ml(-1) were observed.
本文描述了在酸性条件下，使用三氟乙酸（TFA）和三氟乙酸酐（TFAA）的混合物，从 3-炔基-2-氨基吡啶合成 7-氮杂吲哚。该方法成功合成了十五个 7-氮杂吲哚，其中大多数在 2-位和 5-位带有取代基。大多数 7-氮杂吲哚都进行了针对一系列细菌和酵母的抗菌活性测试。7-氮杂吲哚对酵母表现出最好的活性，特别是对新型隐球菌，其活性低至 3.9μgml(-1)。
