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      An insight on medicinal attributes of 1,2,4-triazoles

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          There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.

          Abstract

          The present review aims to summarize the pharmacological profile of 1,2,4-triazole, one of the emerging privileged scaffold, as antifungal, antibacterial, anticancer, anticonvulsant, antituberculosis, antiviral, antiparasitic, analgesic and anti-inflammatory agents, etc. along with structure-activity relationship. The comprehensive compilation of work carried out in the last decade on 1,2,4-triazole nucleus will provide inevitable scope for researchers for the advancement of novel potential drug candidates having better efficacy and selectivity.

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          Highlights

          • •

            1,2,4-Triazole derivatives possess promising potential in drug designing and development.

          • •

            Advances in biological activities in the last decade of 1,2,4-triazole as privileged structure.

          • •

            Plausible mode of action and biomolecular targets for therapeutic potential.

          • •

            Emphasis on structure-activity relationship.

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          Most cited references236

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          Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.

          Ruth Lehr, Philip Harris, Scott B Berger … (2017)
          RIP1 regulates necroptosis and inflammation and may play an important role in contributing to a variety of human pathologies, including immune-mediated inflammatory diseases. Small-molecule inhibitors of RIP1 kinase that are suitable for advancement into the clinic have yet to be described. Herein, we report our lead optimization of a benzoxazepinone hit from a DNA-encoded library and the discovery and profile of clinical candidate GSK2982772 (compound 5), currently in phase 2a clinical studies for psoriasis, rheumatoid arthritis, and ulcerative colitis. Compound 5 potently binds to RIP1 with exquisite kinase specificity and has excellent activity in blocking many TNF-dependent cellular responses. Highlighting its potential as a novel anti-inflammatory agent, the inhibitor was also able to reduce spontaneous production of cytokines from human ulcerative colitis explants. The highly favorable physicochemical and ADMET properties of 5, combined with high potency, led to a predicted low oral dose in humans.
          Article 0 comments Cited 162 times – based on 0 reviews     Review now
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            A century of fungicide evolution

            P. E. RUSSELL (2005)
            Article 0 comments Cited 80 times – based on 0 reviews     Review now
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              Triazole derivatives and their antiplasmodial and antimalarial activities

              Xue-Mei Chu, Cong Wang, Wen-Ling Wang … (2019)
              Article 0 comments Cited 47 times – based on 0 reviews     Review now
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                Author and article information

                Contributors
                Ranjana Aggarwal
                Journal
                Journal ID (nlm-ta): Eur J Med Chem
                Journal ID (iso-abbrev): Eur J Med Chem
                Title: European Journal of Medicinal Chemistry
                Publisher: Elsevier Masson SAS.
                ISSN (Print): 0223-5234
                ISSN (Electronic): 1768-3254
                Publication date PMC-release: 27 July 2020
                Publication date (Electronic): 27 July 2020
                Electronic Location Identifier: 112652
                Affiliations
                [a ]Department of Chemistry, Kurukshetra University, Kurukshetra, 136 119, India
                [b ]CSIR-National Institute of Science Technology and Development Studies, New Delhi, India
                [c ]Department of Chemistry, D. A. V. College (Lahore), Ambala City, 134 003, Haryana, India
                Author notes
                [∗ ]Corresponding author. Department of Chemistry, Kurukshetra University, Kurukshetra, 136 119, India Tel.: +91(1744)238734, +919896740740; fax: +91(1744)238277 ranjanaaggarwal67@ 123456gmail.com
                Article
                Publisher ID: S0223-5234(20)30624-3 Publisher ID: 112652
                DOI: 10.1016/j.ejmech.2020.112652
                PMC ID: 7384432
                PubMed ID: 32771798
                SO-VID: 47e50ac3-787f-4690-a12c-f147c09e388c
                Copyright © © 2020 Elsevier Masson SAS. All rights reserved.
                License:

                Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.

                History
                Date received : 20 June 2020
                Date revision received : 4 July 2020
                Date accepted : 7 July 2020
                Categories
                Subject: Article

                ScienceOpen disciplines: Pharmacology & Pharmaceutical medicine
                Keywords: 1,2,4-triazole,molecular interactions,enzyme inhibitors,hybrid compounds,pharmacological activities,structure-activity relationship
                Data availability:
                ScienceOpen disciplines: Pharmacology & Pharmaceutical medicine
                Keywords: 1,2,4-triazole, molecular interactions, enzyme inhibitors, hybrid compounds, pharmacological activities, structure-activity relationship

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