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SYNTHESIS, AND EVALUATION OF COUMARIN HYBRIDS AS ANTIMYCOBACTERIAL AGENTS

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Hassan M. Z., ALSAYARI A., OSMAN H., ALI M. A., MUHSINAH A. B., AHSAN M. J.

Acta Poloniae Pharmaceutica - Drug Research

2019

vol. 76

issue 6

1029-1036

A series of twelve hybrid coumarin analogues 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]pyrimidine-6-carbonitrile (3f) showed excellent antimycobacterial activity against Mtb (EC50 3.19 & 7.91 µM, respectively) and low cytotoxicity against the VERO cell line (IC50 > 62.5 µg/mL).

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1 Acta Poloniae Pharmaceutica - Drug Research

1 2019

1 AHSAN M. J.

1 ALI M. A.

1 ALSAYARI A.

1 Hassan M. Z.

1 MUHSINAH A. B.

1 OSMAN H.

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SYNTHESIS, AND EVALUATION OF COUMARIN HYBRIDS AS ANTIMYCOBACTERIAL AGENTS