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Article ; Online: Synthesis, Structure–Activity Relationships, and Antiviral Profiling of 1-Heteroaryl-2-Alkoxyphenyl Analogs as Inhibitors of SARS-CoV-2 Replication

Dorothée Bardiot / Laura Vangeel / Mohamed Koukni / Philippe Arzel / Marleen Zwaagstra / Heyrhyoung Lyoo / Patrick Wanningen / Shamshad Ahmad / Linlin Zhang / Xinyuanyuan Sun / Adrien Delpal / Cecilia Eydoux / Jean-Claude Guillemot / Eveline Lescrinier / Hugo Klaassen / Pieter Leyssen / Dirk Jochmans / Karolien Castermans / Rolf Hilgenfeld /
Colin Robinson / Etienne Decroly / Bruno Canard / Eric J. Snijder / Martijn J. van Hemert / Frank van Kuppeveld / Patrick Chaltin / Johan Neyts / Steven De Jonghe / Arnaud Marchand

Molecules, Vol 27, Iss 1052, p

2022  Volume 1052

Abstract: 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 ... ...

Abstract 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 experiments 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.
Keywords COVID-19 ; SARS-CoV-2 ; 1,2,4-oxadiazole ; 1-heteroaryl-2-alkoxyphenyl analogs ; Organic chemistry ; QD241-441
Subject code 540
Language English
Publishing date 2022-02-01T00:00:00Z
Publisher MDPI AG
Document type Article ; Online
Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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