Antimicrobial compounds were synthesized by coupling 4-(4-oxo-3,4-dihydroquinazolin-2-yl) butanoic acid with VP, GVP, VGVP and GVGVP peptides. Antimicrobial activities of the synthesized compounds were performed against various bacterial strains by disc diffusion method. The structure activity relationship was evaluated with respect to hydrophobicity, polarity, chain length of peptides and alkyl chain length of quinazolinone. Correlations of analogs with respect to their antimicrobial activity in comparison with conventional drugs and probable mechanism for the activity were discussed.
A mild and versatile method for the efficient construction of heterocyclic framework of meridianins from simple precursors has been devised. The strategy involves the assembly of the pyrimidine ring utilizing the nucleophilicitiy of monothio-1,3-diketone formed by thioacylation at the C-3 in the indole ring.
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