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新型强效磺胺衍生物的分子建模作为非肽小分子抗 COVID-19 药物。

Molecular modeling of potent novel sulfonamide derivatives as non-peptide small molecule anti-COVID 19 agents.

机构信息

Department of Biological Chemistry, Indian Association for the Cultivation of Science, Kolkata, India.

Department of Chemistry, University of Illinois at Chicago, Chicago, IL, USA.

出版信息

J Biomol Struct Dyn. 2022 Sep;40(15):7129-7142. doi: 10.1080/07391102.2021.1897043. Epub 2021 Jun 1.

Abstract

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the causative agent for the COVID-19. The Sulfonamides groups have been widely introduced in several drugs, especially for their antibacterial activities and generally prescribed for respiratory infections. On the other hand, imidazole groups have the multipotency to act as drugs, including antiviral activity. We have used a structure-based drug design approach to design some imidazole derivatives of sulfonamide, which can efficiently bind to the active site of SARS-CoV-2 main protease and thus may have the potential to inhibit its proteases activity. We conducted molecular docking and molecular dynamics simulation to observe the stability and flexibility of inhibitor complexes. We have checked ADMET (absorption, distribution, metabolism, excretion and toxicity) and drug-likeness rules to scrutinize toxicity and then designed the most potent compound based on computational chemistry. Our small predicted molecule non-peptide protease inhibitors could provide a useful model in the further search for novel compounds since it has many advantages over peptidic drugs, like lower side effects, toxicity and less chance of drug resistance. Further, we confirmed the stability of our inhibitor-complex and interaction profile through the Molecular dynamics simulation study. Our small predicted moleculeCommunicated by Ramaswamy H. Sarma.

摘要

严重急性呼吸系统综合征冠状病毒 2(SARS-CoV-2)是 COVID-19 的病原体。磺胺类药物已广泛应用于多种药物中,特别是因其具有抗菌活性而被广泛应用于呼吸道感染的治疗。另一方面,咪唑基团具有作为药物的多效性,包括抗病毒活性。我们使用基于结构的药物设计方法设计了一些磺胺类咪唑衍生物,它们可以有效地结合到 SARS-CoV-2 主蛋白酶的活性位点,因此可能具有抑制其蛋白酶活性的潜力。我们进行了分子对接和分子动力学模拟,以观察抑制剂复合物的稳定性和灵活性。我们已经检查了 ADMET(吸收、分布、代谢、排泄和毒性)和药物相似性规则,以检查毒性,然后基于计算化学设计最有效的化合物。我们的小分子预测非肽蛋白酶抑制剂可以为进一步寻找新型化合物提供一个有用的模型,因为它与肽类药物相比具有许多优势,如副作用、毒性和耐药性较低的机会。此外,我们通过分子动力学模拟研究证实了我们的抑制剂复合物的稳定性和相互作用模式。我们的小分子预测

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