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用于治疗SARS-CoV-2的拟用抗病毒药物阿匹莫德和粉防己碱中,最具动态活性的甲基的低旋转势垒。

Low rotational barriers for the most dynamically active methyl groups in the proposed antiviral drugs for treatment of SARS-CoV-2, apilimod and tetrandrine.

作者信息

Mamontov Eugene, Cheng Yongqiang, Daemen Luke L, Kolesnikov Alexander I, Ramirez-Cuesta Anibal J, Ryder Matthew R, Stone Matthew B

机构信息

Neutron Scattering Division, Oak Ridge National Laboratory, Oak Ridge, TN 37831, USA.

出版信息

Chem Phys Lett. 2021 Aug 16;777:138727. doi: 10.1016/j.cplett.2021.138727. Epub 2021 May 8.

Abstract

A recent screening study highlighted a molecular compound, apilimod, for its efficacy against the SARS-CoV-2 virus, while another compound, tetrandrine, demonstrated a remarkable synergy with the benchmark antiviral drug, remdesivir. Here, we find that because of significantly reduced potential energy barriers, which also give rise to pronounced quantum effects, the rotational dynamics of the most dynamically active methyl groups in apilimod and tetrandrine are much faster than those in remdesivir. Because dynamics of methyl groups are essential for biochemical activity, screening studies based on the computed potential energy profiles may help identify promising candidates within a given class of drugs.

摘要

最近的一项筛选研究突出了一种分子化合物阿匹莫德对严重急性呼吸综合征冠状病毒2(SARS-CoV-2)病毒的疗效,而另一种化合物粉防己碱则与基准抗病毒药物瑞德西韦表现出显著的协同作用。在此,我们发现,由于势能垒显著降低,这也导致了明显的量子效应,阿匹莫德和粉防己碱中最具动态活性的甲基的旋转动力学比瑞德西韦中的要快得多。由于甲基的动力学对生化活性至关重要,基于计算出的势能分布进行的筛选研究可能有助于在给定的一类药物中识别出有前景的候选药物。

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