Quinazolinone derivatives, which are known for their versatile biological activities, have been reported to show significant antibacterial and antitubercular activities. Fourteen compounds that belong to either 2-methyl substituted quinazolinone or 2-phenyl substituted quinazolinones were synthesized. Compounds 5a-e and 8a-c showed a minimum inhibitory concentration value between 6.25 and 100 µg/mL against Mycobacterium tuberculosis. Compounds 5g and 8d, on the other hand, showed significant antibacterial activity against Staphylococcus albus and Strepto coccus pyogenes. The use of amido, thioamido, imidamido, N,N-dimethyl guanidinyl, or N-pyridoyl substituents at 3-position of quinazolinone was found to increase antitubercular activity. A binding affinity prediction by autodock vina was higher for the 2-phenyl series, which may be due to increased hydrophobic interactions within the binding site of enoyl-acyl carrier protein reductase.

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