Synthesis and antitubercular evaluation of imidazo[2,1-b][1,3,4]thiadiazole derivatives

In the present study, a series of imidazo[2,1-b][1,3,4]thiadiazole derivatives 5(a–j) were synthesized and characterized by IR, 1H NMR, 13C NMR and mass spectral technique. The compounds were evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv strain by usin...

Full description

Saved in:
Bibliographic Details
Published in:Arabian journal of chemistry 2017-02, Vol.10 (S1), p.S996-S1002
Main Authors: Patel, Harun M., Noolvi, Malleshappa N., Sethi, Navdeep Singh, Gadad, Andanappa K., Cameotra, Swaranjit Singh
Format: Article
Language:English
Subjects:
Antitubercular activity
Imidazo[2,1-b][1,3,4]thiadiazole synthesis
Mycobacterium tuberculosis
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:In the present study, a series of imidazo[2,1-b][1,3,4]thiadiazole derivatives 5(a–j) were synthesized and characterized by IR, 1H NMR, 13C NMR and mass spectral technique. The compounds were evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv strain by using Alamar Blue susceptibility test as part of the TAACF TB screening program under direction of the US National Institutes of Health, the NIAID division. Among the tested compounds, 2-(1-methyl-1H-imidazol-2-yl)-6-(4-nitrophenyl)imidazo[2,1-b][1,3,4]thiadiazole (5f) has shown the highest (98%) inhibitory activity with MIC of 3.14μg/ml as compared to other tested compounds. Further, some potent compounds were also assessed for their cytotoxic activity against a mammalian Vero cell line using MTT assay. The results reveal that these compounds exhibit anti-tubercular activity at non-cytotoxic concentrations.
ISSN:1878-5352
1878-5379
DOI:10.1016/j.arabjc.2013.01.001