Description
Title: Dihydroquinazolinone Derivatives: Antitubercular, Cytotoxicity, and Computational Target Validation
Abstract: In order to find compounds with whole-cell antitubercular activity against the tubercular strain H37Rv and MDR Mycobacterium tuberculosis (MTB) strains, a series of 2,3-dihydroquinazolin-4(1H)-one derivatives (3a-3m) were tested. The MTB strain H37Rv was resistant to compounds 3l and 3m with di-substituted aryl moiety (halogens) attached to the 2-position of the scaffold at a concentration as low as 2 g/mL. With MIC values of 4 and 16 g/mL, respectively, compound 3k with an imidazole ring at the 2-position of the dihydroquinazolin-4(1H)-one also exhibited significant inhibitory action against the MDR strains and the susceptible strain H37Rv. The mycobacterial pyridoxal-phosphate (PLP)-dependent aminotransferase (BioA) enzyme was identified as a potential target by the computational analysis. The test compounds 3k-3m were found to be safe and tolerable when tested in vitro on normal human dermal fibroblast cells using ADMET calculations and cytotoxicity studies. In order to create novel BioA inhibitors for the treatment of drug-sensitive H37Rv and drug-resistant MTB, compounds 3k–3m need to be further optimized.
Keywords: dihydroquinazolin-4(1H)-ones; anti-TB activity; MTT assay; molecular docking studies; molecular dynamic simulations studies
Paper Quality: SCOPUS / Web of Science Level Research Paper
Subject: Antibiotics
Writer Experience: 20+ Years
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