AI Article Synopsis

  • Various substituted compounds were successfully synthesized using an efficient methodology, including 5,6-dihydro-8-methoxybenzo[h]quinazolin-2-amine and 2,6-diarylpyridine derivatives.
  • The synthesized compounds were tested for their effectiveness against the Mycobacterium tuberculosis H37Rv strain, with several showing notable anti-tubercular activity.
  • Among these, compound 19a demonstrated significant activity while also being safe, exhibiting a much lower MIC value compared to its cytotoxicity in THP-1 cells.

Article Abstract

Various substituted 5,6-dihydro-8-methoxybenzo[h]quinazolin-2-amine, 1-(3-(4-alkoxyphenyl)-7-methoxy-3,3a,4,5-tetrahydro-2H benzo[g]indazol-2-yl)ethanone, pyrazole and 2,6-diarylpyridine derivatives have been synthesized in good yields by an efficient methodology. The synthesized compounds (4-23) were evaluated for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain. Compounds 6a, 6c, 8a, 19a and 19e exhibited significant anti-tubercular activity at MIC values 50, 100, 50, 25 and 100μM concentration. In vitro cytotoxicity data using THP-1 cells indicated that most active compound 19a is safe as its MIC value is much lower than the cytotoxic value.

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Source
http://dx.doi.org/10.1016/j.bmcl.2013.08.101DOI Listing

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