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新型 N-吡啶基腙衍生物的设计、合成与生物评价作为潜在的单胺氧化酶(MAO)抑制剂。

Design, Synthesis and Biological Evaluation of Novel N-Pyridyl-Hydrazone Derivatives as Potential Monoamine Oxidase (MAO) Inhibitors.

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Aden University, 6075 Aden, Yemen.

出版信息

Molecules. 2018 Jan 8;23(1):113. doi: 10.3390/molecules23010113.

Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/49b2/6017090/e2acf5e4f2ba/molecules-23-00113-g001.jpg

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