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- Title
Antimycobacterial Evaluation and Microwave-Assisted Synthesis of N-(5-methyl-4-oxo-2-arylthiazolidin-3-yl) Isonicotinamide Derivatives.
- Authors
Alghamdi, Saad; Almehmadi, Mazen M.; Asif, Mohammad; Alshehri, Mohammed M.; Kamal, Mehnaz
- Abstract
Thiazolidinone derivatives represent heterocyclic bioactive compounds. We have synthesized some N-(5-methyl-4-oxo-2-arylthiazolidin-3-yl)-isonicotinamide derivatives (2a–2h) from isoniazid (INH) and screened them as antimycobacterial agents against M. tuberculosis H37Rv strain using microplate alamar blue assay (MABA). Compounds 2a-2h were obtained via cyclocondensation of N-arylideneisonicotinohydrazide derivatives (imine Schiff's bases) 1a-1h with thiolactic acid. Initial compounds 1a-1h were synthesized by reaction of isoniazid with appropriate benzaldehyde. The structures of title compounds were established by IR, 1H NMR, and mass spectroscopy data. All the title compounds (2a-2h) exhibited antimycobacterial activity and were compared to standard drugs streptomycin (MIC value of 6.25 μg/mL) and isoniazid (MIC value of 3.125 μg/mL). Compound 2g exhibited the highest antimycobacterial activity, but all the tested compounds were less active than standard drugs.
- Subjects
SCHIFF bases; MASS spectrometry; DRUG standards; ISONIAZID; BIOACTIVE compounds; NICOTINAMIDE
- Publication
Pharmaceutical Chemistry Journal, 2022, Vol 56, Issue 2, p215
- ISSN
0091-150X
- Publication type
Article
- DOI
10.1007/s11094-022-02623-0