Umarani, W. A.

Discovery of selective and potent anti-tubercular activity in arylpentane-1,4-diones - Vol.61(4), Apr - New Delhi CSIR 2022 - 411-415p.

Anti-tubercular activity (MIC 50µg/mL against Mtb H37Rv) have been reported in hispolons, which possess α, β-unsaturated-1,3-diketone functional group. In the pursuit to optimize structure and bioactivity, various substituted arylpentane-1,4-diones S1-8 have been synthesised. Upon screening, the test compounds show negligible antimicrobial activity against the tested organisms at 100 µg/mL but show antitubercular activity against Mycobacterium tuberculosis H37Rv strain with an MIC 0.8 to 25µg/mL. Compounds having a halogen at the ortho position on the aromatic ring show highest potency (MIC 0.8µg/mL), implying a relation between the position of the halogen atom and anti-tubercular activity.


GENERAL CHEMISTRY
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