Peptidomimetic α-Acyloxymethylketone Warheads with Six-Membered Lactam P1 Glutamine Mimic: SARS-CoV-2 3CL Protease Inhibition, Coronavirus Antiviral Activity, and in Vitro Biological Stability-Reference-Cited by-同舟云学术

Peptidomimetic α-Acyloxymethylketone Warheads with Six-Membered Lactam P1 Glutamine Mimic: SARS-CoV-2 3CL Protease Inhibition, Coronavirus Antiviral Activity, and in Vitro Biological Stability

Published:2021-07-09 Issue: Volume: Page:
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Bai Bing¹²,Belovodskiy Alexandr¹²,Hena Mostofa¹²,Kandadai Appan Srinivas¹²,Joyce Michael A.³²,Saffran Holly A.³²,Shields Justin A.³²,Khan Muhammad Bashir⁴,Arutyunova Elena³⁴,Lu Jimmy³⁴,Bajwa Sardeev K.⁴,Hockman Darren¹²,Fischer Conrad⁵,Lamer Tess⁵,Vuong Wayne⁵^ORCID,van Belkum Marco J.⁵,Gu Zhengxian⁶,Lin Fusen⁶,Du Yanhua⁶,Xu Jia⁶,Rahim Mohammad⁷,Young Howard S.⁴,Vederas John C.⁵^ORCID,Tyrrell D. Lorne¹³²,Lemieux M. Joanne³⁴^ORCID,Nieman James A.¹²^ORCID

Affiliation:

1. Li Ka Shing Applied Virology Institute, University of Alberta, Edmonton, Alberta T6G 2E1, Canada

2. Department of Medical Microbiology and Immunology, University of Alberta, Edmonton, Alberta T6G 2E1, Canada

3. Li Ka Shing Institute of Virology, University of Alberta, Edmonton, Alberta T6G 2E1, Canada

4. Department of Biochemistry, University of Alberta, Edmonton, Alberta T6G 2H7, Canada

5. Department of Chemistry, University of Alberta, Edmonton, Alberta T6G 2G2, Canada

6. WuXi AppTec (Shanghai) Co., Ltd., G Warehouse #101, No. 10 Building, #227 Meisheng Road, WaiGaoQiao Free Trade Zone, Shanghai 200131, China

7. Rane Pharmaceuticals, Inc. 4290 91a Street NW, Edmonton, Alberta T6E 5V2, Canada

Funder

Canadian Institutes of Health Research

Alberta Innovates

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.1c00616

Reference75 articles.

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3. Structure-Based Design, Synthesis, and Biological Evaluation of Irreversible Human Rhinovirus 3C Protease Inhibitors. 4. Incorporation of P1 Lactam Moieties as l-Glutamine Replacements

4. Center for Disease Control and Prevention. https://www.cdc.gov/norovirus/trends-outbreaks/worldwide.html (accessed 2021-02-06).

5. COVID-19: Drug Targets and Potential Treatments

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