The synthesis of ethyl 4-oxo-1,4-dihydroquinoline-3-carboxylates (4, 5) was performed via the reaction of corresponding anilines with diethyl ethoxymethylenemalonate under conventional and also microwave promoted conditions. The treatment of 4 and 5 afforded the corresponding hydrazides (6 and 7). These hydrazides were converted to the corresponding carbo(thio)amides (9a-f and 10a-e) which were then subjected to an intramolecular cyclisation leading to the formation of quinolone-triazole hybrids (11a-f and 12a-e). The newly synthesized compounds were screened for their biological activities such as antioxidant capacity (AC) and acetylcholinesterase Activity. Inhibition of cholinesterases is an effective method to curb Alzheimer’s disease, a progressive and fatal neurological disorder. A series of some novel quinolone derivatives were designed, synthesized, and their inhibitory effects on AChE were evaluated. We obtained our compounds and determined their anticholinesterase activities according to the Ellman’s method. 9b and 10c showed the best AChE inhibition with 0.48 ± 0.02 and 0.52 ± 0.07, respectively. Docking studies were performed for the most active compounds (9b, 10c) and interaction modes with enzyme active sites were determined. As a result of these studies, a strong interaction between these compounds and the active sites of AChE enzyme was revealed.

4-氧代-1,4-二氢喹啉-3-羧酸盐（合成4，5通过相应的苯胺的反应的常规和微波也促进的条件下进行用二乙氧基亚甲基）。4和5的处理得到相应的酰肼（6和7）。这些酰肼被转化为相应的碳（硫）酰胺（9a-f和10a-e），然后进行分子内环化，形成喹诺酮-三唑杂化物（11a-f和12a-e）。）。筛选新合成的化合物的生物活性，例如抗氧化能力（AC）和乙酰胆碱酯酶活性。抑制胆碱酯酶是遏制阿尔茨海默氏病（一种进行性和致命性神经系统疾病）的有效方法。设计，合成了一系列新颖的喹诺酮衍生物，并评价了其对AChE的抑制作用。我们获得了我们的化合物，并根据Ellman方法确定了它们的抗胆碱酯酶活性。图9b和10c显示了最佳的AChE抑制，分别为0.48±0.02和0.52±0.07。对活性最高的化合物（9b，10c）进行了对接研究），并确定了与酶活性位点的相互作用方式。这些研究的结果表明，这些化合物与AChE酶的活性位点之间具有很强的相互作用。