Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Aden University, 6075 Aden, Yemen.
Molecules. 2018 Jan 8;23(1):113. doi: 10.3390/molecules23010113.
A new series of -pyridyl-hydrazone derivatives was synthesized by using a simple and efficient method. The final compounds obtained were screened for their inhibitory potency against monoamine oxidase (MAO) A and B. The newly synthesized compounds - specifically inhibited monoamine oxidases, displaying notably low IC values. Compounds and , with a CF₃ and OH group on the 4-position of the phenyl ring, respectively, showed considerable MAO-A and MAO-B inhibitory activities. Compounds , and , with -methylpyrrole, furan and pyridine moieties instead of the phenyl ring, were the most powerful and specific inhibitors of MAO-A, with IC values of 6.12 μM, 10.64 μM and 9.52 μM, respectively. Moreover, these active compounds were found to be non-cytotoxic to NIH/3T3 cells. This study supports future studies aimed at designing MAO inhibitors to obtain more viable medications for neurodegenerative disorders, such as Parkinson's disease.
用一种简单有效的方法合成了一系列新的 -吡啶基腙衍生物。最终得到的化合物被筛选其对单胺氧化酶（MAO）A 和 B 的抑制活性。新合成的化合物 - 特异性抑制单胺氧化酶，显示出明显低的 IC 值。化合物 和 ，在苯环的 4-位上分别有 CF₃ 和 OH 基团，表现出相当强的 MAO-A 和 MAO-B 抑制活性。化合物 、 和 ，用 -甲基吡咯、呋喃和吡啶取代苯环，是 MAO-A 的最强和最特异抑制剂，IC 值分别为 6.12 μM、10.64 μM 和 9.52 μM。此外，这些活性化合物对 NIH/3T3 细胞没有细胞毒性。这项研究支持旨在设计 MAO 抑制剂以获得更可行的治疗神经退行性疾病（如帕金森病）药物的未来研究。
