Abstract

A novel N²-alkyl-3-thioxo-8-nitro-1,2,4-triazino[5,6-b]indoles and 3-alkylated 3-thioxo-8-nitro-1,2,4-triazino[5,6-b]indoles (2–13) were obtained by treatment of 8-nitro-1,2,4-triazino[5,6-b]indole-3-(2H,5H)thione (1) using various alkylating agents and different regioselective conditions. The chemical reactivity of compound 1 toward some nucleophilic and electrophilic compounds such as isothiocyanates, primary amines, and sulfonamides was investigated. The structures of the synthesized compounds were confirmed by spectral data and elemental analysis. The biological activity of the new compounds was tested and revealed the promising antibacterial activity of 6, 8, and 4 were when Ampicillin was used as a reference.

摘要

一种新型的N ² -alkyl-3-thioxo-8-nitro-1,2,4-triazino[5,6- b ]indoles 和 3-烷基化 3-thioxo-8-nitro-1,2,4-triazino[ 5,6- b ]indoles ( 2–13 ) 是通过 8-nitro-1,2,4-triazino[5,6- b ]indole-3-(2 H, 5 H )thione ( 1 )处理得到的使用各种烷化剂和不同的区域选择性条件。化合物1的化学反应性研究了一些亲核和亲电化合物，例如异硫氰酸酯、伯胺和磺胺。通过光谱数据和元素分析证实了合成化合物的结构。对这些新化合物的生物活性进行了测试，结果表明当以氨苄青霉素为参考时，6、8和4具有良好的抗菌活性。