作为广谱抗病毒剂的3-炔基-5-芳基-7-氮杂吲哚的合成与评价
Synthesis and evaluation of 3-alkynyl-5-aryl-7-aza-indoles as broad-spectrum antiviral agents.
作者信息
Martinez-Gualda Belén, Graus Mirthe, Camps Anita, Vanhulle Emiel, Saul Sirle, Azari Siavash, Nhu Tran Do Hoang, Vangeel Laura, Chiu Winston, Neyts Johan, Schols Dominique, Einav Shirit, Vermeire Kurt, De Jonghe Steven
机构信息
KU Leuven, Department of Pharmaceutical and Pharmacological Sciences, Rega Institute for Medical Research, Laboratory of Medicinal Chemistry, Leuven, Belgium.
KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium.
出版信息
Front Chem. 2022 Oct 26;10:1058229. doi: 10.3389/fchem.2022.1058229. eCollection 2022.
RNA viral infections, including those caused by respiratory syncytial virus (RSV), severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), and Venezuelan Equine encephalitis virus (VEEV), pose a major global health challenge. Here, we report the synthesis and screening of a series of pyrrolo[2,3-]pyridines targeting RSV, SARS-CoV-2 and/or VEEV. From this campaign, a series of lead compounds was generated that demonstrated antiviral activity in the low single-digit micromolar range against the various viruses and did not show cytotoxicity. These findings highlight the potential of 3-alkynyl-5-aryl-7-aza-indoles as a promising chemotype for the development of broad-spectrum antiviral agents.
包括由呼吸道合胞病毒（RSV）、严重急性呼吸综合征冠状病毒2（SARS-CoV-2）和委内瑞拉马脑炎病毒（VEEV）引起的感染在内的RNA病毒感染，构成了一项重大的全球健康挑战。在此，我们报告了一系列针对RSV、SARS-CoV-2和/或VEEV的吡咯并[2,3 -]吡啶的合成与筛选。通过这项研究，产生了一系列先导化合物，它们对各种病毒表现出低个位数微摩尔范围内的抗病毒活性，并且未显示出细胞毒性。这些发现突出了3 - 炔基 - 5 - 芳基 - 7 - 氮杂吲哚作为开发广谱抗病毒药物的一种有前景的化学类型的潜力。
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