Abstract The present paper elicits a marvelous synthesis of a series of sulfonamide containing 1,4-disubstituted 1,2,3-triazoles through click reaction of terminal alkynes with aromatic azides. The synthesized triazoles were characterized by FTIR, 1H NMR,13C NMR and HRMS techniques. Further, the structures of synthesized compounds 6u (CCDC 1954932) and 6z3 (CCDC 1954931) were also confirmed by X-ray crystallography. The synthesized triazoles were evaluated for in vitro antibacterial activity against S. aureus, B.subtilis, E. coli and K. pneumoniae by serial dilution method. Among the series, compound 4-bromo-N-(2-(1-(4-bromophenyl)-1H-1,2,3-triazol-4-yl)propan-2-yl)benzenesulfonamide, 6z4 (MIC = 0.025 µM/mL) and 4-bromo-N-(2-(1-(naphthalen-1-yl)-1H-1,2,3-triazol-4-yl)propan-2-yl)benzenesulfonamide 6z6 (MIC = 0.027 µM/mL) exhibited the appreciable antibacterial activity against Staphylococcus aureus and Bacillus subtilis. Further, the molecular docking studies of above potent analogs with dihydropteroate synthase was performed to have an insight for binding interactions. Synthesized molecules were also explored for antioxidant activity, reflecting compound 6m as better radical scavenging agent with IC50 value of 1.96 µM/mL. Graphical Abstract

中文翻译：

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磺胺标记的 1,2,3-三唑类化合物的合成、表征和生物活性

摘要 本文通过末端炔烃与芳香叠氮化物的点击反应，成功合成了一系列含1,4-二取代1,2,3-三唑的磺酰胺。通过FTIR、1H NMR、13C NMR和HRMS技术对合成的三唑类化合物进行了表征。此外，合成的化合物6u（CCDC 1954932）和6z3（CCDC 1954931）的结构也通过X射线晶体学证实。通过连续稀释法评价合成的三唑类化合物对金黄色葡萄球菌、枯草芽孢杆菌、大肠杆菌和肺炎克雷伯菌的体外抗菌活性。该系列中，化合物4-溴-N-(2-(1-(4-溴苯基)-1H-1,2,3-三唑-4-基)丙-2-基)苯磺酰胺，6z4 (MIC = 0.025 µM/mL) 和 4-溴-N-(2-(1-(naphthalen-1-yl)-1H-1,2,3-triazol-4-yl)propan-2-yl) 苯磺酰胺 6z6 (MIC = 0. 027 µM/mL) 对金黄色葡萄球菌和枯草芽孢杆菌表现出明显的抗菌活性。此外，对上述具有二氢蝶酸合酶的强效类似物进行了分子对接研究，以深入了解结合相互作用。还研究了合成分子的抗氧化活性，表明化合物 6m 作为更好的自由基清除剂，IC50 值为 1.96 µM/mL。图形概要