Bacterial drug resistance has become a growing problem worldwide due to the excessive use of antibiotics in recent decades. Two small focused libraries of 5H-pyrimido[5,4-b]indole-4-carboxamides and 5H-pyrimido-[5,4-b]indole-4-ketones were designed as eudistomin Y₃ and 1-acetyl-β-carboline (1-ABC) analogs and prepared via application of Inverse Electron-Demand Diels-Alder (IEDDA) reaction of 1,3,5-triazines and 3-aminoindoles. Compounds 2a and 2b were discovered to have activity against Mycobacterium bovis BCG with Minimum Inhibitory Concentration (MICs) values of 25 and 50 μg/mL respectively while compound 2e was against all three strains of Candida albicans tested with MIC values of 50 μg/mL. Moreover, compound 2e demonstrated synergistic antibacterial activity with fluconazol, which suggested that future drug candidates from this class of compounds could be used in combination with existing drugs to treat C. albicans infections.

由于近几十年来抗生素的过度使用，细菌耐药性已成为世界范围内日益严重的问题。5 H -pyrimido[5,4 - b ]indole-4-carboxamides 和 5 H -pyrimido- [5,4 - b ]indole-4-ketones 的两个小型聚焦文库被设计为eudistomin Y ₃和1-乙酰- β-咔啉(1-ABC)类似物，通过应用 1,3,5-三嗪和 3-氨基吲哚的逆电子需求狄尔斯-阿尔德 (IEDDA) 反应制备。发现化合物2a和2b对牛分枝杆菌具有活性BCG 的最小抑制浓度 (MIC) 值分别为 25 和 50 μg/mL，而化合物2e对所有三种白色念珠菌菌株均具有 50 μg/mL 的 MIC 值。此外，化合物2e显示出与氟康唑的协同抗菌活性，这表明此类化合物的未来候选药物可与现有药物联合用于治疗白色念珠菌感染。