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Design, synthesis and biological evaluation of novel spiro-[chroman-2,4 '-piperidin]-4-one analogs as anti-tubercular agents

Journal Contribution - e-publication

A series of novel spiro-[chromane-2,4'-piperidin]-4(3H)-one derivatives were designed, synthesized and structures were confirmed by analytical methods, viz., H-1-NMR, C-13-NMR and mass spectrometry. The synthetic derivatives were evaluated for their anti-tuberculosis (anti-TB) activity against Mycobacterium tuberculosis (Mtb) strain H37Ra. Among all the evaluated Compounds, PS08 exhibited significant inhibition with MIC value of 3.72 mu M while MIC values of the remaining Compounds ranged from 7.68 to 230.42 mu M in comparison to the standard drug INH (MIC 0.09 mu M). The two most active Compounds however showed acute cytotoxicity towards the human MRC-5 lung fibroblast cell lines. The in silico ADMET profiles of the titled Compounds were predicted and found within the prescribed limits of the Lipinski and Jorgenson rules. Molecular docking study of the notably active Compound (PS08) was also carried out after performing validation in order to understand the putative binding position of the test ligand at the active site of selected target protein Mtb tyrosine phosphatase (PtpB).
Journal: Chemistry & biodiversity
ISSN: 1612-1872
Volume: 19
Pages: 1 - 9
Publication year:2022
Keywords:A1 Journal article