Background: There is a great need to discover more drugs with antimycobacterial activities to fight lung cancer and tuberculosis (two of the deadliest diseases worldwide). To our knowledge, the present study is the first to report the antimycobacterial activity of imidazole-fused heterocycles.

Objective: Construction of some bis-imidazole fused heterocycles with potential anti-tubercular and/or potent antitumor activities.

Methods: A series of bis-imidazole fused derivatives 6-8 and 13-16 was constructed using bisphenacyl bromide derivative 2 as a synthetic platform. Compound 2 was also used to access bisquinoxaline 20, bis-benzothiazine derivatives 23, and bis-thiazolopyrimidine derivatives 26. The new bis-imidazole derivatives were evaluated for their anticancer activity against the lung carcinoma cell line (A-549) using Cisplatin as a reference drug. The new compounds were also screened for their anti-tubercular activity against M. tuberculosis (ATCC 25177) using Isoniazid as a reference drug.

Results: Among the new bis-imidazole derivatives, three examples showed remarkable antitumor activities while five other compounds showed high antimycobacterial activity.

Conclusion: A novel series of bis-imidazole fused heterocycles was developed. Multiple prototypes of this new series showed remarkable anti-tubercular and/or potent antitumor activities.

背景：迫切需要发现更多具有抗分枝杆菌活性的药物来对抗肺癌和肺结核（世界上最致命的两种疾病）。据我们所知，本研究首次报道了咪唑稠合杂环的抗分枝杆菌活性。

目的：构建一些具有潜在抗结核和/或有效抗肿瘤活性的双咪唑稠合杂环。

方法：以双苯甲酰溴衍生物2为合成平台，构建了一系列双咪唑稠合衍生物6-8和13-16。化合物 2 还用于获取双喹喔啉 20、双苯并噻嗪衍生物 23 和双噻唑并嘧啶衍生物 26。使用顺铂作为新的双咪唑衍生物对肺癌细胞系 (A-549) 的抗癌活性进行了评估参考药物。还使用异烟肼作为参考药物筛选了新化合物对结核分枝杆菌 (ATCC 25177) 的抗结核活性。

结果：在新的双咪唑衍生物中，三个实例显示出显着的抗肿瘤活性，而其他五个化合物显示出较高的抗分枝杆菌活性。

结论：开发了一系列新型双咪唑稠合杂环。这个新系列的多个原型显示出显着的抗结核和/或有效的抗肿瘤活性。