Literature DB >> 31951961

Synthesis and antimycobacterial activity of thiazolidine-2,4-dione based derivatives with halogenbenzohydrazones and pyridinecarbohydrazones substituents.

Nazar Trotsko1, Joanna Golus2, Paulina Kazimierczak2, Agata Paneth3, Agata Przekora2, Grazyna Ginalska2, Monika Wujec3.   

Abstract

The two series of thiazolidine-2,4-dione (TZD) based hybrids with halogenbenzohydrazones and pyridinecarbohydrazones substituents were designed and synthesized. Target hydrazones were evaluated for their antimycobacterial activity by broth microdilution method with resazurin as an indicator of the metabolic activity of mycobacteria. Conducted studies revealed antimycobacterial activity in the concentration range of 1-512 μg/ml for 23 synthesized TZD-based derivatives. The highest antimycobacterial activity (MIC = 1 μg/ml) was demonstrated for the new group of compounds: TZD-based derivatives with pyridine-4-carbohydrazone substituent. Furthermore, all the tested compounds within this group were characterized by low cytotoxicity. On the basis of the results obtained, three compounds with the highest SI were selected. High effectiveness and safety of these synthesized derivatives makes them promising candidates as antimycobacterial agents.
Copyright © 2020 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Antimycobacterial activity; Cytotoxicity; Mycobacterium tuberculosis H37Ra; Pyridinecarbohydrazones; Thiazolidine-2,4-dione based hybrids; Tuberculosis

Year:  2020        PMID: 31951961     DOI: 10.1016/j.ejmech.2020.112045

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  4 in total

Review 1.  The Bioactivity of Thiazolidin-4-Ones: A Short Review of the Most Recent Studies.

Authors:  Dominika Mech; Antonina Kurowska; Nazar Trotsko
Journal:  Int J Mol Sci       Date:  2021-10-26       Impact factor: 5.923

2.  Synthesis, biological evaluation and in-silico ADME studies of novel series of thiazolidin-2,4-dione derivatives as antimicrobial, antioxidant and anticancer agents.

Authors:  Harsh Kumar; Davinder Kumar; Pradeep Kumar; Suresh Thareja; Minakshi Gupta Marwaha; Umashanker Navik; Rakesh Kumar Marwaha
Journal:  BMC Chem       Date:  2022-09-15

Review 3.  Thiazolidin-2,4-Dione Scaffold: An Insight into Recent Advances as Antimicrobial, Antioxidant, and Hypoglycemic Agents.

Authors:  Harsh Kumar; Navidha Aggarwal; Minakshi Gupta Marwaha; Aakash Deep; Hitesh Chopra; Mohammed M Matin; Arpita Roy; Talha Bin Emran; Yugal Kishore Mohanta; Ramzan Ahmed; Tapan Kumar Mohanta; Muthupandian Saravanan; Rakesh Kumar Marwaha; Ahmed Al-Harrasi
Journal:  Molecules       Date:  2022-10-10       Impact factor: 4.927

4.  In Vitro Antimycobacterial Activity and Physicochemical Characterization of Diaryl Ether Triclosan Analogues as Potential InhA Reductase Inhibitors.

Authors:  Tarek S Ibrahim; Ehab S Taher; Ebtihal Samir; Azizah M Malebari; Ahdab N Khayyat; Mamdouh F A Mohamed; Riham M Bokhtia; Mohammed A AlAwadh; Israa A Seliem; Hani Z Asfour; Nabil A Alhakamy; Siva S Panda; Amany M M Al-Mahmoudy
Journal:  Molecules       Date:  2020-07-08       Impact factor: 4.411

  4 in total

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