Discovery of selective and potent anti-tubercular activity in arylpentane-1,4-diones

Abstract

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.