(E)-3,4-dihydroxystyryl alkyl sulfones, as new analogues of neurodegenerative agents, were designed and synthesized. The biological results demonstrated that most of the target compounds preserved antioxidant and anti-inflammatory potency in scavenging reactive free radicals, protecting neuronal cells against neurotoxins such as H₂O₂, 6-hydroxydopamine and inhibiting lipopolysaccharide (LPS)-induced over-production of NO. Among these compounds, 6.22 with cyclopentyl propyl exhibited prominent antioxidant activity at low concentration (2.5 μM) in H₂O₂ model (cell viability = 94.5%). In addition, 6.22 (IC₅₀ = 1.6 μM) displayed better anti-inflammatory activity than that of lead compound 1 (IC₅₀ = 13.4 μM). In view of the outstanding performance of 6.22, the apoptotic rates of H₂O₂-damaged PC12 cells were detected by Annexin V-FITC/PI assay. 6.22 showed higher potency in inhibition of apoptosis than 1 at low concentration (2.5 μM), consisting with the antioxidant and anti-inflammatory models. Furthermore, with the predicted CNS (+) blood-brain barrier (BBB) permeability (P_e = 6.84 × 10⁻⁶ cm s⁻¹), low cytotoxicity and favorable physiochemical properties based on calculation, compound 6.22 can be further developed as a potential multifunctional neuroprotective agent.

设计并合成了（E）-3,4-二羟基苯乙烯基烷基砜，作为神经变性剂的新类似物。生物结果表明，大部分目标化合物在清除活性自由基保留的抗氧化和抗炎效力，保护神经元细胞免于神经毒素如H ₂ ö ₂，6-羟基和抑制脂多糖（LPS）诱导的过度产生的不。在这些化合物中，6.22在低浓度（2.5环戊基丙基展出突出的抗氧化活性 μ H中M）₂ ö ₂模型（细胞活力= 94.5％）。此外，6.22（IC ₅₀ = 1.6  μ M）显示比铅化合物的更好的抗炎活性1（IC ₅₀  = 13.4  μ M）。鉴于6.22的优异性能，通过膜联蛋白V-FITC / PI测定法检测了H ₂ O ₂损伤的PC12细胞的凋亡率。6.22显示出更高效力在抑制细胞凋亡比1 在低浓度（2.5  μ M），其由与抗氧化剂和抗炎模型。此外，在具有预测的CNS（+）血脑屏障（BBB）渗透性的情况下（P _e  = 6.84×10 ^-6  cm s ^-1），低细胞毒性和良好的理化性质（基于计算），化合物6.22可以进一步开发为潜在的多功能神经保护剂。