Design, synthesis and biological evaluation of novel oxindole analogs as antitubercular agents

To design, synthesize and evaluate oxindole derivatives for antitubercular activity. We synthesized the derivatives, confirmed their structures by H/ C NMR and mass spectrometry, and evaluated them for antitubercular activity against H37Rv strain using the microplate alamarBlue™ assay. Among all the...

Full description

Saved in:
Bibliographic Details
Published in:Future medicinal chemistry 2023-08, Vol.15 (15), p.1323-1342
Main Authors: Khetmalis, Yogesh M, Sangeetha, Guruvelli PV, Chandu, Ala, Swati, Murugesan, Sankaranarayanan, Sharma, Vivek, Kumar, Muthyala MK, Kondapalli, Venkata GCS
Format: Article
Language:English
Subjects:
hybridization
molecular docking
nitrofuran
oxindole
tuberculosis
Citations: Items that this one cites
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:To design, synthesize and evaluate oxindole derivatives for antitubercular activity. We synthesized the derivatives, confirmed their structures by H/ C NMR and mass spectrometry, and evaluated them for antitubercular activity against H37Rv strain using the microplate alamarBlue™ assay. Among all the synthesized derivatives, , and exhibited excellent antitubercular activity (minimum inhibitory concentration [MIC]: 0.78 μg/ml). Compounds with a MIC ≤1.56 were tested for cytotoxicity against human embryonic kidney cells and were found to be relatively nontoxic. Molecular docking analysis of , and was performed to determine their binding patterns at the active site of DNA topoisomerase II (PDB-5BS8). In drug combination studies, , and showed synergism with isoniazid. The obtained results reveal that oxindole derivatives exhibit potent antitubercular activity.
ISSN:1756-8919
1756-8927
DOI:10.4155/fmc-2023-0066