Khattab Sherine Nabil, Bekhit Adnan Ahmed, El-Faham Ayman, El Massry Abdel Moneim, Amer Adel
Department of Chemistry, Faculty of Science, University of Alexandria, Alexandria, Egypt.
Chem Pharm Bull (Tokyo). 2008 Dec;56(12):1717-21. doi: 10.1248/cpb.56.1717.
A series of new pyridazinylacetic acid derivatives were synthesized and have been investigated for their ability to inhibit the activity of the A and B isoforms of monoamine oxidase (MAO). All compounds were found to be more selective to the MAO-A isoform with compound 5d having the highest SI values. Computational study performed with a docking technique indicated the potential of these compounds in pyridazine-based MAO-A inhibitor drug development.
合成了一系列新的哒嗪基乙酸衍生物，并对其抑制单胺氧化酶（MAO）A和B同工型活性的能力进行了研究。发现所有化合物对MAO-A同工型具有更高的选择性，其中化合物5d的选择性指数（SI）值最高。采用对接技术进行的计算研究表明，这些化合物在基于哒嗪的MAO-A抑制剂药物开发中具有潜力。
