Alkyne Derivatives of SARS-CoV-2 Main Protease Inhibitors Including Nirmatrelvir Inhibit by Reacting Covalently with the Nucleophilic Cysteine

Author:

Brewitz Lennart1ORCID,Dumjahn Leo1,Zhao Yilin1,Owen C. David23ORCID,Laidlaw Stephen M.4,Malla Tika R.1ORCID,Nguyen Dung4,Lukacik Petra23,Salah Eidarus1,Crawshaw Adam D.2ORCID,Warren Anna J.2ORCID,Trincao Jose2,Strain-Damerell Claire23,Carroll Miles W.4,Walsh Martin A.23ORCID,Schofield Christopher J.1ORCID

Affiliation:

1. Chemistry Research Laboratory, Department of Chemistry and the Ineos Oxford Institute for Antimicrobial Research, University of Oxford, 12 Mansfield Road, Oxford OX1 3TA, United Kingdom

2. Diamond Light Source Ltd., Harwell Science and Innovation Campus, Didcot OX11 0DE, United Kingdom

3. Research Complex at Harwell, Harwell Science and Innovation Campus, Didcot OX11 0FA, United Kingdom

4. Wellcome Centre for Human Genetics, Nuffield Department of Medicine, University of Oxford, Oxford OX3 7BN, United Kingdom

Funder

Oak Foundation

University of Oxford

King Abdulaziz University

Wellcome Trust

Biotechnology and Biological Sciences Research Council

Cancer Research UK

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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