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• W2328046009 abstract "2-Styrylquinazolones are reported as a novel class of potent anti-mycobacterial agents. Forty-six target compounds have been synthesized using one pot reaction involving isatoic anhydride, amine, and triethyl orthoacetate followed by aldehyde to construct the 2-styrylquinazolone scaffold. The anti-mycobacterial potency of the compounds was determined against H37Rv strain. Twenty-six compounds exhibited anti-Mtb activity in the range of 0.40-6.25μg/mL. Three compounds 8c, 8d and 8ab showed MIC of 0.78μg/mL and were found to be non-toxic (<50% inhibition at 50μg/mL) to HEK 293T cell lines with the therapeutic index >64. The most potent compound 8ar showed MIC of 0.40μg/mL with the therapeutic index >125. An early structure activity relationship for this class of compounds has been established. The computational studies indicate the possibility of these compounds binding to the penicillin binding proteins (PBPs)." @default.
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• W2328046009 date "2016-06-01" @default.
• W2328046009 modified "2023-10-16" @default.
• W2328046009 title "Synthesis, biological evaluation and structure–activity relationship of 2-styrylquinazolones as anti-tubercular agents" @default.
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• W2328046009 doi "https://doi.org/10.1016/j.bmcl.2016.04.012" @default.
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