- Tytuł:
- SYNTHESIS, AND EVALUATION OF COUMARIN HYBRIDS AS ANTIMYCOBACTERIAL AGENTS
- Autorzy:
-
Hassan, Mohd Z.
ALSAYARI, ABDULRHMAN
OSMAN, HASNAH
ALI, MOHAMED A.
MUHSINAH, ABDULLATIF B.
AHSAN, MOHAMED J. - Powiązania:
- https://bibliotekanauki.pl/articles/895509.pdf
- Data publikacji:
- 2019-12-29
- Wydawca:
- Polskie Towarzystwo Farmaceutyczne
- Tematy:
-
cytotoxicity
Coumarin
TB
Thiazolopyrimidine
HTS
antimycobacterial - Opis:
- 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).
- Źródło:
-
Acta Poloniae Pharmaceutica - Drug Research; 2019, 76, 6; 1029-1036
0001-6837
2353-5288 - Pojawia się w:
- Acta Poloniae Pharmaceutica - Drug Research
- Dostawca treści:
- Biblioteka Nauki
Artykuł