Literature DB >> 28712709

Synthesis and biological evaluation of novel 1,2,3-triazole derivatives as anti-tubercular agents.

Abdul Aziz Ali1, Dhrubajyoti Gogoi2, Amrita K Chaliha2, Alak K Buragohain2, Priyanka Trivedi3, Prakash J Saikia4, Praveen S Gehlot5, Arvind Kumar5, Vinita Chaturvedi6, Diganta Sarma7.   

Abstract

A library of seventeen novel 1,2,3-triazole derivatives were efficiently synthesized in excellent yields by the popular 'click chemistry' approach and evaluated in vitro for their anti-tubercular activity against Mycobacterium tuberculosis H37Ra (ATCC 25177 strain). Among the series, six compounds exhibited significant activity with minimum inhibitory concentration (MIC) values ranging from 3.12 to 0.78μg/mL and along with no significant cytotoxicity against MBMDMQs (mouse bone marrow derived macrophages). Molecular docking of the target compounds into the active site of DprE1 (Decaprenylphosphoryl-β-d-ribose-2'-epimerase) enzyme revealed noteworthy information on the plausible binding interactions.
Copyright © 2017 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  1,2,3-Triazoles; Antimycobacterial activity; Cytotoxicity; Molecular docking; Tuberculosis

Mesh:

Substances:

Year:  2017        PMID: 28712709     DOI: 10.1016/j.bmcl.2017.07.008

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


  6 in total

1.  Synthesis, antibacterial activity and molecular docking study of vanillin derived 1,4-disubstituted 1,2,3-triazoles as inhibitors of bacterial DNA synthesis.

Authors:  Mumtaz Hussain; Tahir Qadri; Zahid Hussain; Aamer Saeed; Pervaiz Ali Channar; Syeda Aaliya Shehzadi; Mubashir Hassan; Fayaz Ali Larik; Tarique Mahmood; Arif Malik
Journal:  Heliyon       Date:  2019-11-19

2.  Design and Synthesis of Novel Imidazole Derivatives Possessing Triazole Pharmacophore with Potent Anticancer Activity, and In Silico ADMET with GSK-3β Molecular Docking Investigations.

Authors:  Fawzia Al-Blewi; Salma Akram Shaikh; Arshi Naqvi; Faizah Aljohani; Mohamed Reda Aouad; Saleh Ihmaid; Nadjet Rezki
Journal:  Int J Mol Sci       Date:  2021-01-25       Impact factor: 5.923

Review 3.  An Overview on the Performance of 1,2,3-Triazole Derivatives as Corrosion Inhibitors for Metal Surfaces.

Authors:  Meryem Hrimla; Lahoucine Bahsis; My Rachid Laamari; Miguel Julve; Salah-Eddine Stiriba
Journal:  Int J Mol Sci       Date:  2021-12-21       Impact factor: 5.923

4.  Design, synthesis, biological evaluation and molecular docking study of novel pyridoxine-triazoles as anti-Alzheimer's agents.

Authors:  Tiyas Pal; Saipriyanka Bhimaneni; Abha Sharma; S J S Flora
Journal:  RSC Adv       Date:  2020-07-09       Impact factor: 4.036

5.  Design, synthesis, and activity of 2-aminochromone core N,N-bis-1,2,3-triazole derivatives using click chemistry.

Authors:  Jayaprakash Rao Yerrabelly; Subbanarasimhulu Porala; Venkateshwar Reddy Kasireddy; Earrawandla Janapriya Sony; Someshswar Rao Sagurthi
Journal:  Chem Zvesti       Date:  2022-09-05       Impact factor: 2.146

Review 6.  Triazole analogues as potential pharmacological agents: a brief review.

Authors:  Sachin Kumar; Sukhbir Lal Khokra; Akash Yadav
Journal:  Futur J Pharm Sci       Date:  2021-05-25
  6 in total

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