Abstract
A series of twelve hybrid coumarin analogs were synthesized and screened through HTS for their antimycobacterial activity against Mtb H37Rv. The hybrid molecules were efficiently synthesized by the reactions of 3-(bromoacetyl)coumarin with Biginelli products 2-mercapto-6-oxo-4-aryl-1,6-dihydropyrimidine-5-carbonitriles. Of the resulting twelve hybrids, the two compounds 7-(2,4-dichlorophenyl)-5-oxo-3-(2-oxo-2H-chromen-3-yl)-5H-thiazolo[3,2-a] pyrimidine-6-carbonitrile (3d) and 7-(4-nitrophenyl)-5-oxo-3-(2-oxo-2H-chromen-3-yl)-5H-thiazolo[3,2-a]pyrirnidine-6-carboniaile (3f) showed excellent antimycobacterial activity against Mg, (EC50 3.19 & 7.91 mu M, respectively) and low cytotoxicity against the VERO cell line (IC50 > 62.5 mu g/mL).