Jump to main content
Jump to site search

Issue 3, 2017
Previous Article Next Article

Design, synthesis, molecular-docking and antimycobacterial evaluation of some novel 1,2,3-triazolyl xanthenones

Author affiliations

Abstract

As part of an ongoing effort to develop new antitubercular and antimicrobial agents, a series of substituted xanthenone derivatives (7a–p) were synthesized. Xanthenone derivatives (7a–p) were prepared via a one-pot three-component thermal cyclization reaction of β-naphthol (5), substituted 1-aryl-1H-[1,2,3]triazole-4-carbaldehydes (4a–h), and cyclic-1,3-diones (6a, b) in the presence of a catalytic amount of iodine. The newly synthesized compounds were characterized by IR, NMR, mass spectral data, and elemental analysis. These compounds (4a–h and 7a–p) were screened for in vitro antitubercular activity against the M. tuberculosis H37Rv (ATCC 27294) strain, for antibacterial activity against Gram-positive and Gram-negative strains, and for antifungal activity against a pathogenic strain of fungi. Among the compounds tested, most of them showed good to excellent antimicrobial and antitubercular activity. The active compounds displaying good potency in the MTB were further examined for toxicity in a HEK cell line. In addition, the structure and antitubercular activity relationship were further supported by in silico molecular-docking studies of the active compounds against the pantothenate synthetase (PS) enzyme of M. tuberculosis.

Graphical abstract: Design, synthesis, molecular-docking and antimycobacterial evaluation of some novel 1,2,3-triazolyl xanthenones

Back to tab navigation
Please wait while Download options loads

Supplementary files

Publication details

The article was received on 27 Oct 2016, accepted on 26 Dec 2016, published on 03 Jan 2017 and first published online on 03 Jan 2017


Article type: Research Article
DOI: 10.1039/C6MD00593D
Citation: Med. Chem. Commun., 2017,8, 559-570
  •   Request permissions

    Design, synthesis, molecular-docking and antimycobacterial evaluation of some novel 1,2,3-triazolyl xanthenones

    G. L. Goud, S. Ramesh, D. Ashok, V. P. Reddy, P. Yogeeswari, D. Sriram, B. Saikrishna and V. Manga, Med. Chem. Commun., 2017, 8, 559
    DOI: 10.1039/C6MD00593D

Search articles by author