2008•Journal of Enzyme Inhibition and Medicinal ChemistryOpen access

Synthesis and antimycobacterial activity of 4-[5-(substituted phenyl)-4, 5-dihydro-3-isoxazolyl]-2-methylphenols

Mohammad Shahar Yar, Mohamed Ashraf Ali, Md. Afroz Bakht, Vel Murugan

Abstract

Compounds based on the isoxazoline moiety were screened for their antimycobacterial activity in vitro against Mycobacterium tuberculosis H37R (MTB), and INH (isoniazid) resistant Mycobacterium tuberculosis (INHR-MTB) using the agar dilution method and bactec 460. Among the synthesized compounds, 4-[5-(4-bromophenyl)-4,5-dihydro-3-isoxazolyl]-2-methylphenol (4l) was found to be the most active agent against MTB and INHR-MTB with minimum inhibitory concentration of 0.62 microM. When compared to INH, compound (4l) was 1.12 fold and 3.0 fold more active against MTB and INHR-MTB, respectively.

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Key concepts: Antimycobacterial, Isoniazid, Mycobacterium tuberculosis, Moiety, Minimum inhibitory concentration, Agar dilution, Chemistry, In vitro