Antifungal activities of (E)-4-benzylidene-5-oxopyrrolidine- 2-carboxamides and 6-oxo-1,2,3,6-tetrahydropyridin-2- carboxamides synthezed via ugi reaction from baylis-hillman bromides

2nd International Conference on Agricultural and Biological Sciences

农业科学;生物科学

Zeng, X.H.^1 ; Xiang, L.C.^1 ; Li, H.L.^1 ; Wang, H.M.^1 ; Wang, X.B.^1

Laboratory of Chinese Herbal Pharmacology, Renmin Hospital, Hubei University of Medicine, Shiyan

442000, China^1

关键词: Anti-fungal activity;    Anti-HIV activity;    Baylis-Hillman;    Biological properties;    Gibberella zeae;    Inhibition rate;    Inhibitory effect;    Regioselective synthesis;   

Others  :  https://iopscience.iop.org/article/10.1088/1755-1315/41/1/012017/pdf
DOI  :  10.1088/1755-1315/41/1/012017

来源: IOP

【 摘 要 】

The derivatives of N-containing heterocycles containing the pyrrolidone or pyridinone moiety are of high importance because they have extensive biological properties including antifungal, anti-muscarinic, anti-cancer, anti-viral and anti-HIV activities. In our previous work, we described an one-pot transition-metal-free, base-mediated synthesis of pyrrolidinones ((E)-4-benzylidene-5-oxopyrrolidine-2-carboxamides 6) and an one-pot regioselective synthesis of previously seldom reported pyridinones (6-oxo-1,2,3,6- tetrahydropyridin-2-carboxamides 9) via Ugi reaction from Baylis-Hillman Bromides. Herein, the growth inhibitory effect of one concentration (50mg/L) of compounds 6 and 9 against fungi (Gibberella zeae) in vitro was tested by the method of toxic medium. Ihe results showed that the inhibitory effects of compounds 6 against Gibberella zeae are not obvious, but compounds 9 showed moderate to good inhibitory effects against Gibberella zeae. Compound 9h showed the best inhibition rate against Gibberella zeae with 95%.