Design, Synthesis, and Biological Evaluation of Trisubstituted Piperazine Derivatives as Noncovalent Severe Acute Respiratory Syndrome Coronavirus 2 Main Protease Inhibitors with Improved Antiviral Activity and Favorable Druggability-Reference-Cited by-同舟云学术

Design, Synthesis, and Biological Evaluation of Trisubstituted Piperazine Derivatives as Noncovalent Severe Acute Respiratory Syndrome Coronavirus 2 Main Protease Inhibitors with Improved Antiviral Activity and Favorable Druggability

Published:2023-11-22 Issue:23 Volume:66 Page:16426-16440
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Gao Shenghua¹²,Song Letian¹,Sylvester Katharina³,Mercorelli Beatrice⁴^ORCID,Loregian Arianna⁴^ORCID,Toth Karoly⁵,Weiße Renato H.⁶^ORCID,Useini Abibe⁶^ORCID,Sträter Norbert⁶^ORCID,Yang Mianling¹,Ye Bing¹,Tollefson Ann E.⁵,Müller Christa E.³^ORCID,Liu Xinyong¹^ORCID,Zhan Peng¹^ORCID

Affiliation:

1. Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Ji’nan 250012, China

2. Shenzhen Research Institute of Shandong University, A301 Virtual University Park in South District of Shenzhen, Shenzhen, Guangdong 518057, PR China

3. PharmaCenter Bonn & Pharmaceutical Institute, Department of Pharmaceutical & Medicinal Chemistry, University of Bonn, An der Immenburg 4, 53113 Bonn, Germany

4. Department of Molecular Medicine, University of Padua, Via Gabelli 63, 35121 Padua, Italy

5. Department of Molecular Microbiology and Immunology, Saint Louis University School of Medicine, St. Louis, Missouri 63103, United States

6. Institute of Bioanalytical Chemistry, Center for Biotechnology and Biomedicine, Leipzig University, Deutscher Platz 5, Leipzig 04103, Germany

Funder

European Commission

Associazione Italiana per la Ricerca sul Cancro

Basic and Applied Basic Research Foundation of Guangdong Province

Ministero dell'Universit? e della Ricerca

Fondazione Cassa di Risparmio di Padova e Rovigo

Natural Science Foundation of Shandong Province

Science Fund for Distinguished Young Scholars of Shandong Province

Universit? degli Studi di Padova

Volkswagen Foundation

Foreign Cultural and Educational Experts Project

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.3c01876

Reference30 articles.

1. A pneumonia outbreak associated with a new coronavirus of probable bat origin

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3. Structural plasticity of SARS-CoV-2 3CL Mpro active site cavity revealed by room temperature X-ray crystallography

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5. Medicinal chemistry strategies towards the development of effective SARS-CoV-2 inhibitors

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