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      Discovery of Novel Cysteine Protease Inhibitors for the Treatment of Coronavirus (COVID-19)

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          Abstract

          The application describes compounds, such as compounds of general Formula, with warheads and their use in treating medical diseases or disorders, such as viral infections. Pharmaceutical compositions and synthetic methods of various compounds with warheads are included. The compounds are inhibitors of proteases, such as the 3C, CL- or 3CL-like protease.

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          Targeting SARS-CoV-2 Proteases and Polymerase for COVID-19 Treatment: State of the Art and Future Opportunities

          Rolando Cannalire, Carmen Cerchia, Andrea R Beccari … (2020)
          The newly emerged coronavirus, called SARS-CoV-2, is the causing pathogen of pandemic COVID-19. The identification of drugs to treat COVID-19 and other coronavirus diseases is an urgent global need, thus different strategies targeting either virus or host cell are still under investigation. Direct-acting agents, targeting protease and polymerase functionalities, represent a milestone in antiviral therapy. The 3C-like (or Main) protease (3CLpro) and the nsp12 RNA-dependent RNA-polymerase (RdRp) are the best characterized SARS-CoV-2 targets and show the highest degree of conservation across coronaviruses fostering the identification of broad-spectrum inhibitors. Coronaviruses also possess a papain-like protease, another essential enzyme, still poorly characterized and not equally conserved, limiting the identification of broad-spectrum agents. Herein, we provide an exhaustive comparative analysis of SARS-CoV-2 proteases and RdRp with respect to other coronavirus homologues. Moreover, we highlight the most promising inhibitors of these proteins reported so far, including the possible strategies for their further development.
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            Protease targeted COVID-19 drug discovery and its challenges: Insight into viral main protease (Mpro) and papain-like protease (PLpro) inhibitors

            Sk. Abdul Amin, Suvankar Banerjee, Kalyan Ghosh … (2020)
            Highlight • Prorteases (Mpro and PLpro) are part of the replication machinery of corona virus. • Mpro and PLpro inhibitors may serve as therapeutic weapons against SARS-CoV-2. • An exquisite picture of the recent coronavirus protease inhibitors is provided. • Experimental screening approaches are also highlighted. • Challenges in the development of effective as well as drug like protease inhibitors is also discussed.
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              The SARS‐CoV‐2 main protease (M pro): Structure, function, and emerging therapies for COVID‐19

              Qing Hu, Yuan Xiong, Guang-Hao Zhu … (2022)
              The main proteases (M pro ), also termed 3‐chymotrypsin‐like proteases (3CL pro ), are a class of highly conserved cysteine hydrolases in β‐coronaviruses. Increasing evidence has demonstrated that 3CL pro s play an indispensable role in viral replication and have been recognized as key targets for preventing and treating coronavirus‐caused infectious diseases, including COVID‐19. This review is focused on the structural features and biological function of the severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) main protease M pro (also known as 3CL pro ), as well as recent advances in discovering and developing SARS‐CoV‐2 3CL pro inhibitors. To better understand the characteristics of SARS‐CoV‐2 3CL pro inhibitors, the inhibition activities, inhibitory mechanisms, and key structural features of various 3CL pro inhibitors (including marketed drugs, peptidomimetic, and non‐peptidomimetic synthetic compounds, as well as natural compounds and their derivatives) are summarized comprehensively. Meanwhile, the challenges in this field are highlighted, while future directions for designing and developing efficacious 3CL pro inhibitors as novel anti‐coronavirus therapies are also proposed. Collectively, all information and knowledge presented here are very helpful for understanding the structural features and inhibitory mechanisms of SARS‐CoV‐2 3CL pro inhibitors, which offers new insights or inspiration to medicinal chemists for designing and developing more efficacious 3CL pro inhibitors as novel anti‐coronavirus agents. A comprehensive summary of recent advances in SARS‐CoV‐2 3CL pro inhibitors (including marketed drugs, peptidomimetic, and non‐peptidomimetic synthetic compounds, as well as natural compounds and their derivatives), including the inhibitory activities, inhibitory mechanisms, and key structural features, provides new insights for designing and developing more efficacious 3CL pro inhibitors as broad‐spectrum anti‐coronavirus agents.
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                Author and article information

                Journal
                Journal ID (nlm-ta): Curr Med Chem
                Journal ID (iso-abbrev): Curr Med Chem
                Journal ID (publisher-id): CMC
                Title: Current Medicinal Chemistry
                Publisher: Bentham Science Publishers
                ISSN (Print): 0929-8673
                ISSN (Electronic): 1875-533X
                Publication date (Electronic): 23 October 2024
                Publication date (Print): 23 October 2024
                Volume: 31
                Issue: 9
                Pages: 1165-1169
                Affiliations
                [1 ]Department of Chemistry, Conju-Probe , San Diego, , California , USA;
                [2 ]deptDepartment of Chemistry , Bharath University , Chennai, , Tamil Nadu, , 600126 , India
                Author notes
                [* ]Address correspondence to this author at the Department of Chemistry, Conju-Probe, San Diego, California, USA; E-mail: desurya125@ 123456gmail.com
                Article
                Publisher ID: CMC-31-1165
                DOI: 10.2174/0929867330666230519163305
                PMC ID: 10788913
                PubMed ID: 37211851
                SO-VID: bb893464-4e06-49de-b587-c4faa84ee909
                Copyright © © 2024 Bentham Science Publishers
                License:

                © 2024 The Author(s). Published by Bentham Science Publisher. This is an open access article published under CC BY 4.0 https://creativecommons.org/licenses/by/4.0/legalcode)

                History
                Date received : 11 February 2023
                Date revision received : 09 April 2023
                Date accepted : 19 April 2023
                Categories
                Subject: Medicine, Immunology, Inflammation & Allergy, Chemistry, Medicinal Chemistry, Pharmacology, Biochemistry and Molecular Biology

                ScienceOpen disciplines: Pharmaceutical chemistry
                Keywords: cysteine protease inhibitors,covid-19,cysteine proteases,3c-like protease,paxlovid,molnupiravir
                Data availability:
                ScienceOpen disciplines: Pharmaceutical chemistry
                Keywords: cysteine protease inhibitors, covid-19, cysteine proteases, 3c-like protease, paxlovid, molnupiravir

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