39123-45-0Relevant academic research and scientific papers
Synthesis, Structure–Activity Relationships, and Antiviral Profiling of 1-Heteroaryl-2-Alkoxyphenyl Analogs as Inhibitors of SARS-CoV-2 Replication
Ahmad, Shamshad,Arzel, Philippe,Bardiot, Dorothée,Canard, Bruno,Castermans, Karolien,Chaltin, Patrick,De Jonghe, Steven,Decroly, Etienne,Delpal, Adrien,Eydoux, Cecilia,Guillemot, Jean-Claude,Hilgenfeld, Rolf,Jochmans, Dirk,Klaassen, Hugo,Koukni, Mohamed,Lescrinier, Eveline,Leyssen, Pieter,Lyoo, Heyrhyoung,Marchand, Arnaud,Neyts, Johan,Robinson, Colin,Snijder, Eric J.,Sun, Xinyuanyuan,Vangeel, Laura,Wanningen, Patrick,Zhang, Linlin,Zwaagstra, Marleen,van Hemert, Martijn J.,van Kuppeveld, Frank
, (2022/02/11)
The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the causative agent of COVID-19, has led to a pandemic, that continues to be a huge public health burden. Despite the availability of vaccines, there is still a need for small-molecule antiviral drugs. In an effort to identify novel and drug-like hit matter that can be used for subsequent hit-to-lead optimization campaigns, we conducted a high-throughput screening of a 160 K compound library against SARS-CoV-2, yielding a 1-heteroaryl-2-alkoxyphenyl analog as a promising hit. Antiviral profiling revealed this compound was active against various beta-coronaviruses and preliminary mode-of-action experi-ments demonstrated that it interfered with viral entry. A systematic structure–activity relationship (SAR) study demonstrated that a 3-or 4-pyridyl moiety on the oxadiazole moiety is optimal, whereas the oxadiazole can be replaced by various other heteroaromatic cycles. In addition, the alkoxy group tolerates some structural diversity.
NOVEL 1,2,4 OXADIAZOLE COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 73, (2009/12/28)
The invention relates to 1,2,4 oxadiazole compounds and analogs thereof, represented by formula (II), and compositions and methods of use thereof.
