Design, Synthesis and Anti-tubercular Evaluation of Some Novel Chroman-Hydrazone Derivatives

Abstract

The molecular docking, synthesis, spectral characterization and anti-tubercular evaluation of 10 novel N'-substituted-6-hydroxy-2,5,7,8-tetramethylchroman-2-carbohydrazide derivatives (SM1-SM10) were reported. The structures of the synthesized derivatives were affirmed by spectroscopic studies such as FTIR, 1H NMR, 13C NMR and high resolution-mass spectrometry. Predicted ADME and toxicity investigations were accomplished to presume the pharmacokinetic parameters of the compounds. The synthesized compounds were evaluated for in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain using Microplate Alamar Blue Assay (MABA) taking isoniazid, rifampicin, ethambutol, amikacin, streptomycin and levofloxacin as positive drug standards. Compound SM8 has shown the significant anti-tubercular activity among all the titled compounds. The results indicated that chroman-hydrazone skeleton could serve as a lead for the development of novel anti-tubercular drugs. © 2023 Chemical Publishing Co.. All rights reserved.