New 1,2,3-triazolo(thieno)stilbenes were synthesized by Wittig reaction and photochemically transformed to corresponding substituted thienobenzo/naphtho-triazoles in high isolated yields. They were prepared to study the acetyl- and butyrylcholinesterase inhibition associated with the inhibition of TNFα cytokine production and anti-inflammatory activity. The best experimental results were achieved with the allyl-thienobenzotriazole and isopropyl, p-methoxybenzyl, and hydroxybutyl substituted naphthotriazoles bearing additional chloro or methoxy groups. The allyl-thienobenzotriazole photoproduct is twice as potent an inhibitor of eqBChE compared to the standard galantamine. At the same time, this compound strongly inhibited TNFα production in PBMCs in response to the LPS stimulus. The complexes between selected compounds with the active site of BChE and AChE are assessed by docking, providing insight into the stabilizing interactions between the potential inhibitor and the active site.

通过 Wittig 反应合成了新的 1,2,3-三唑并(噻吩)二苯乙烯，并以高分离产率光化学转化为相应的取代噻吩苯并/萘并三唑。他们准备研究与抑制 TNF α细胞因子产生和抗炎活性相关的乙酰胆碱酯酶和丁酰胆碱酯酶抑制。最好的实验结果是用烯丙基噻吩并苯并三唑和异丙基，p-甲氧基苄基和羟基丁基取代的萘并三唑，带有额外的氯或甲氧基。与标准加兰他敏相比，烯丙基-噻吩并苯并三唑光产物是 eqBChE 抑制剂的两倍。同时，该化合物响应 LPS 刺激强烈抑制 PBMC 中 TNFα 的产生。通过对接评估所选化合物与 BChE 和 AChE 活性位点之间的复合物，从而深入了解潜在抑制剂和活性位点之间的稳定相互作用。