Design, Synthesis, and Antimicrobial Activity of Novel 6-Oxopyrimidin-1(6H)-yl Benzamide Derivatives

被引:0
作者
K. Devarasetty
J. Vantikommu
J. Sh. Anireddy
P. Srinivas
机构
[1] Chemistry Services Unit,Centre for Chemical Sciences and Technology
[2] GVK Biosciences Pvt. Ltd,undefined
[3] IDA Nacharam,undefined
[4] Institute of Science and Technology,undefined
[5] JNT University Hyderabad,undefined
来源
Russian Journal of General Chemistry | 2019年 / 89卷
关键词
Pyrimidones; oxadiazolo[3,2-; ]pyrimidin-5-ol; oxadiazolo[3,2-; ]pyrimidin-5-one; antibacterial activity; antifungal activity;
D O I
暂无
中图分类号
学科分类号
摘要
A series of novel 1-(benzamide)-N-cyclopropyl-2-(amino substituted)-6-oxo-1,6-dihydropyrimidine-5-carboxamide derivatives is synthesised and characterized by IR, 1H and 13C NMR, and mass spectra. The synthesized compounds 6a-6j and 8a-8j are screened for their in vitro antimicrobial activity against two Grampositive (Staphylococcus aureus, Bacillus subtilis) and two Gram-negative bacteria (Escherichia coli, Klebesiella aerogenes), and two pathogenic fungi (Aspergillus flavus, Fusarium oxysporum). Most of the compounds demonstrate good to excellent antimicrobial activity in comparison with the standard drugs ciproflaxin and hymexazole. Among the screened compounds morpholine substituted dihydropyrimidone carboxamide 8j is determined to be the most potent anti-bacterial agent.
引用
收藏
页码:780 / 788
页数:8
相关论文
共 63 条
[1]  
Jones ED(2010)undefined Bioorg. Med. Chem. Lett. 20 5913-undefined
[2]  
Vandegraaff N(2010)undefined Bioorg. Med. Chem. Lett. 20 5909-undefined
[3]  
Le G(2008)undefined Bioorg. Med. Chem. 16 7102-undefined
[4]  
Choi N(2010)undefined Eur. J. Med. Chem. 45 738-undefined
[5]  
Issa W(2006)undefined Eur. J. Med. Chem. 41 833-undefined
[6]  
Macfarlane K(2008)undefined Chinese Chem. Lett. 19 669-undefined
[7]  
Thienthong N(1999)undefined Cancer 85 2265-undefined
[8]  
Winfield LJ(1967)undefined Dokl. Akad. Nauk. SSSR 176 332-undefined
[9]  
Coates JA(1968)undefined Quart. Rev. 22 934-undefined
[10]  
Lu L(2012)undefined Res. Pharm. 2 1-undefined