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

By: Umarani, W. A.
Contributor(s): Sony, K. P.
Publisher: New Delhi CSIR 2022Edition: Vol.61(4), Apr.Description: 411-415p.Subject(s): GENERAL CHEMISTRYOnline resources: Click here In: Indian journal of chemistry (Section B)Summary: 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.
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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.

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