A new class of structurally intriguing heterocycles embedded with spiropyrrolidine, oxindole and chromanones was prepared by regio- and stereoselectively in quantitative yields using an intermolecular tandem cycloaddition protocol. The compounds synthesized were assayed for their anti-mycobacterial activity against () H37Rv and isoniazid-resistant ( and promoter mutations) clinical isolates. Four compounds exhibited significant antimycobacterial activity against strains tested. In particular, a compound possessing a fluorine substituted derivative displayed potent activity at 0.39 μg mL against H37Rv, while it showed 0.09 μg mL and 0.19 μg mL activity against promoter and mutation isolates, respectively. A molecular docking study was conducted with the potent compound, which showed results that were consistent with the experiments.
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11008671 | PMC |
http://dx.doi.org/10.1039/d4ra01501k | DOI Listing |
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