1. Synthesis and biological screening of thiosemicarbazones of substituted 3-acetylcoumarins having d-glucose moiety.
- Author
-
Ngoc Toan, Vu, Dinh Thanh, Nguyen, Minh Tri, Nguyen, and Thi Thu Huong, Nguyen
- Subjects
- *
THIOSEMICARBAZONES , *BIOSYNTHESIS , *MOIETIES (Chemistry) - Abstract
• Ten new thiosemicarbazones of substituted 3-acetylcoumarins with d -glucose moiety were synthesized in 45–68% yields. • Several thiosemicarbazones were active against Gram-(+) and Gram-(−) bacteria with MICs of 1.56–3.125 μM. • Some thiosemicarbazones had activity against fungi with MICs of 1.56–3.125 μM. • Compounds 5h and 5i exhibited excellent activity against S. aureus with MIC of 0.78 μM. • Compounds exhibited excellent activity with MIC of 0.78 μM, including 5h (for C. albicans), and 5i (for S. cerevisiae). Thiosemicarbazones 5a-j were synthesized with yields of 45–68% by condensation of 3-acetylcoumarins 3a-j and tetra- O -acetyl-β- d -thiosemicarbazide 4. All obtained thiosemicarbazones were screened for anti-microorganic activities against bacteria (B. subtilis , S. aureus , S. epidermidis , E. coli , P. aeruginosa , K. pneumoniae , S. typhimurium) and fungi (A. niger , C. albicans , S. cerevisiae , and A. flavus). Some compounds had significant inhibitory activity with MICs of 0.78–3.125 μM in comparison with 5a , including 5e , h , i for S. aureus , and 5c , f , i for S. epidermidis (Gram-(+) bacteria), 5c , f , g for E.coli , 5f for K. pneumoniae , 5b , c , g for P. aeruginosa , and 5i for S. typhimurium (Gram-(−) bacteria), 5d , h , i for A. niger , 5i for A. flavus , 5b , d , e , h for C. albicans , and 5i for S. cerevisiae. Compounds exhibited excellent activity against tested microorganism with MIC = 0.78 μM, including 5h,i (against S. aureus), 5h (against C. albicans), and 5i (against S. cerevisiae). [ABSTRACT FROM AUTHOR]
- Published
- 2020
- Full Text
- View/download PDF