The aim of this study was to investigate the antibacterial and acetylcholinesterase (AChE) inhibitory activities of 3-(3-(2/3/4-substituted phenyl)triaz-1-en-1-yl)benzenesulfonamides (compounds 1 – 12) and to find out new possible drug candidate molecules since the available agents in clinical use have some limitations. According to the results of antibacterial screening for compounds 1 – 12, most of the synthesized compounds were found to be effective against Gram-positive microorganisms while being ineffective (MIC > 1600 μg/mL) on Gram-negative microorganisms. According to the AChE inhibition results, K_i values of compounds 1 – 12 were in the range of 5 ± 1 – 34 ± 2 nMtoward AChE. Tacrine (TAC) used as a reference drug had K_i value of 4 ± 1 nM toward AChE. The non-substituted derivative compound 1 coluld be considered as a lead compound for this study in terms of AChE inhibitory activity, since its K_i value (5 ± 1 nM) was close to that of the reference drug (TAC). Thus, compound 1 was docked at the binding site of AChE and showed good interaction with the target enzyme, suggesting their possible mechanism of action.

本研究的目的是研究 3-(3-(2/3/4-取代苯基)triaz-1-en-1-yl) 苯磺酰胺（化合物1 – 12）的抗菌和乙酰胆碱酯酶 (AChE) 抑制活性并寻找新的可能的候选药物分子，因为临床使用的可用药物有一些局限性。根据化合物1-12的抗菌筛选结果，发现合成的化合物大部分对革兰氏阳性微生物有效，而对革兰氏阴性微生物无效（MIC > 1600 μg/mL）。根据 AChE 抑制结果，化合物1-12 的K _i值在 5 ± 1 – 34 ± 2 nMtoward AChE 的范围内。用作参考药物的他克林 (TAC)对 AChE 的K _i值为 4 ± 1 nM。就 AChE 抑制活性而言，未取代的衍生化合物1可被视为本研究的先导化合物，因为其K _i值 (5 ± 1 nM) 接近参考药物 (TAC) 的K _i值。因此，化合物1停靠在 AChE 的结合位点，并显示出与目标酶的良好相互作用，表明它们可能的作用机制。