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朝向基于吡唑啉的 MAO 抑制剂的选择性和可逆性发展:合成、生物评估和对接研究。

Towards development of selective and reversible pyrazoline based MAO-inhibitors: Synthesis, biological evaluation and docking studies.

机构信息

Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi 835 215, India.

出版信息

Bioorg Med Chem Lett. 2010 Jan 1;20(1):132-6. doi: 10.1016/j.bmcl.2009.11.015. Epub 2009 Nov 12.

Abstract

Ten novel 3,5-diaryl pyrazolines were synthesized and investigated for their monoamine oxidase (MAO) inhibitory property. All the molecules were found to be reversible and selective inhibitor for either one of the isoform (MAO-A or MAO-B). Further insights in the theoretical evaluation of the possible interactions between the compounds and monoamine oxidases (MAO-A or MAO-B) have been developed through docking studies. The theoretical values are in congruence with their experimental values.

摘要

合成了 10 种新型 3,5-二芳基吡唑啉,并研究了它们对单胺氧化酶(MAO)的抑制作用。所有分子均被发现为 MAO-A 或 MAO-B 同工型的可逆和选择性抑制剂。通过对接研究进一步深入了解了化合物与单胺氧化酶(MAO-A 或 MAO-B)之间可能相互作用的理论评估。理论值与实验值相符。

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