Literature DB >> 32987135

Design and synthesis of new indanol-1,2,3-triazole derivatives as potent antitubercular and antimicrobial agents.

Pramod S Phatak1, Rajubai D Bakale1, Ravibhushan S Kulkarni1, Sambhaji T Dhumal2, Prashant P Dixit3, Vagolu Siva Krishna4, Dharmarajan Sriram4, Vijay M Khedkar5, Kishan P Haval6.   

Abstract

In a search of new antitubercular agents, herein we have reported a series of new thirty-two indanol-1,2,3-triazole derivatives. The synthesized compounds were screened for their in vitro antitubercular and antimicrobial activities. Among the screened compounds, most of the compounds have displayed good antitubercular activity against Mycobacterium tuberculosis H37Rv. The compound 5g has been identified as potent antitubercular agent with MIC value 1.56 µM. The most active compounds of the series were further studied for their cytotoxicity against HEK 293 cells using MTT assay and found to be nontoxic. In addition, ten compounds were shown good antimicrobial activities against both antibacterial and antifungal pathogens. A molecular docking study against Mycobacterial enoyl-ACP-reductase (InhA) was performed to gain an insight into the molecular mechanism of antitubercular action. The pharmacokinetic parameters of these compounds were studied and displayed acceptable drug-likeness score.
Copyright © 2020 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  1,2,3-Triazoles; ADME prediction; Antimicrobial activity; Antitubercular activity; Click chemistry; Molecular docking study

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Year:  2020        PMID: 32987135     DOI: 10.1016/j.bmcl.2020.127579

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Design, Synthesis and Molecular Docking of Novel Acetophenone-1,2,3-Triazoles Containing Compounds as Potent Enoyl-Acyl Carrier Protein Reductase (InhA) Inhibitors.

Authors:  Fawzia Faleh Albelwi; Hanaa M Abdu Mansour; Maram M Elshatanofy; Yeldez El Kilany; Kamal Kandeel; Bassma H Elwakil; Mohamed Hagar; Mohamed Reda Aouad; El Sayed H El Ashry; Nadjet Rezki; Maged A El Sawy
Journal:  Pharmaceuticals (Basel)       Date:  2022-06-27

2.  Synthesis and Antitumor Activity of 1-Substituted 1,2,3-Triazole-Mollugin Derivatives.

Authors:  Han Luo; Yong-Feng Lv; Hong Zhang; Jiang-Miao Hu; Hong-Mei Li; Shou-Jin Liu
Journal:  Molecules       Date:  2021-05-28       Impact factor: 4.411

  2 in total

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