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2019 | 76 | 6 | 1029-1036
Article title

SYNTHESIS, AND EVALUATION OF COUMARIN HYBRIDS AS ANTIMYCOBACTERIAL AGENTS

Content
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EN
Abstracts
EN
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).
Year
Volume
76
Issue
6
Pages
1029-1036
Physical description
Dates
published
2019-12-29
References
Document Type
Publication order reference
Identifiers
YADDA identifier
bwmeta1.element.doi-10_32383_appdr_112406
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