In this study, synthesis of nine N-phenylsulfonamide derivatives was designed by starting from aniline, which is the simplest aromatic amine. These compounds were obtained in yields between 69 and 95%. Inhibitory properties of synthesized compounds on carbonic anhydrase I (CA I), CA II isoenzymes, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes were investigated. Inhibitors of CA isoenzymes are important therapeutic targets, particularly due to their preventive/activation potential in the treatment of diseases such as edema, glaucoma, cancer and osteoporosis. Cholinesterase inhibitors are valuable compounds that can be used in many different therapeutic applications, including Alzheimer's disease. The compound 8 for CA I, AChE and BChE, 2 for CA II showed a very active inhibition profile (K_I 45.7 ± 0.46 for CA I, 33.5 ± 0.38 nM for CA II, 31.5 ± 0.33 nM for AChE and 24.4 ± 0.29 nM for BChE). The results indicate that these N-phenyl-sulfonamide derivatives are potent CA and cholinesterases and new potential drugs.

在这项研究中，从苯胺开始设计了九种N-苯基磺酰胺衍生物的合成，苯胺是最简单的芳香胺。获得这些化合物的产率为69-95％。研究了合成化合物对碳酸酐酶I（CA I），CA II同工酶，乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BChE）酶的抑制特性。CA同功酶抑制剂是重要的治疗靶标，特别是由于它们在治疗诸如水肿，青光眼，癌症和骨质疏松症等疾病中具有预防/激活潜力。胆碱酯酶抑制剂是有价值的化合物，可用于许多不同的治疗应用中，包括阿尔茨海默氏病。化合物8为CA I，乙酰胆碱酯酶和的BChE，2对于CA II表现出非常活跃抑制轮廓（K_我45.7±0.46对CA I，33.5±0.38纳米的CA II，31.5±0.33 nM的对乙酰胆碱酯酶和24.4±0.29纳米的BChE的）。结果表明，这些N-苯基磺酰胺衍生物是有效的CA和胆碱酯酶以及新的潜在药物。