Synthesis of heterocyclic compounds encompassing multiple functionalities and their biological screening is the most adapted strategy in the world for pharmacological evaluation of future drug candidates. The undertaken research was initiated by esterification 2-(1H-indol-3-yl)acetic acid (1) with catalytic amount of sulfuric acid in ethanol to ethyl 2-(1H-indol-3-yl)acetate (2), which was then reacted with hydrazine hydrate in methanol to achieve 2-(1H-indol-3-yl)acetohydrazide (3). The corresponding hydrazide 3 was reacted with a variety of arylsulfonyl chlorides (4a-j) in sodium carbonate solution (pH 9-10) to afford N-[2-(1H-indol-3-yl)acetyl]arylsulfonohydrazides (5a-j). The structural characterization of synthesized compounds was done by ¹H-NMR, ¹³C-NMR, IR and EI-MS spectral data. Moreover, these derivatives were evaluated for anti-bacterial potentials along with their % age hemolytic and enzyme inhibitory activities. It was found that compounds 5a, 5b, 5d and 5h revealed good anti-bacterial against all the bacterial strains used in this study, while 5d, 5g and 5h exhibited good enzyme inhibition potentials against BChE which were close to the reference standard eserine. These compounds also revealed low values of % hemolytic activity. Results of computational docking were also found in agreement with the enzyme inhibition data.

合成包含多种功能的杂环化合物及其生物筛选是世界上对未来候选药物进行药理评估的最合适的策略。所进行的研究是通过在乙醇中用催化量的硫酸将 2-(1 H - indol-3-yl) 乙酸(1)酯化为 2-(1 H - indol-3-yl) 乙酸乙酯(2) 开始的，然后与水合肼在甲醇中反应，得到 2-(1 H -indol-3-yl) 乙酰肼(3)。相应的酰肼3与多种芳基磺酰氯(4a-j)在碳酸钠溶液 (pH 9-10) 中反应得到N- [2-( 1H-吲哚-3-基)乙酰基]芳基磺酰肼(5a-j)。合成化合物的结构表征是通过¹ H-NMR、¹³ C-NMR、IR 和 EI-MS 光谱数据完成的。此外，评估了这些衍生物的抗菌潜力以及它们的溶血百分比和酶抑制活性。发现化合物5a、5b、5d和5h对本研究中使用的所有细菌菌株显示出良好的抗菌作用，而5d、5g和5h对 BChE 表现出良好的酶抑制潜力，接近参考标准丝氨酸。这些化合物还显示出低的溶血活性％值。计算对接的结果也与酶抑制数据一致。