Catalytic synthesis and antimicrobial activity of N-(3-chloro-2-oxo-4-phenylazetidin-1-yl)-4-(1H-indol-3-yl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamides

被引:6
作者
Desai, Nisheeth C. [1 ,2 ]
Bhatt, Malay J. [2 ]
机构
[1] Maharaja Krishnakumarsinhji Bhavnagar Univ, Dept Chem, DST FIST Sponsored, Mahatma Gandhi Campus, Bhavnagar 364002, Gujarat, India
[2] Maharaja Krishnakumarsinhji Bhavnagar Univ, UGC NONSAP, Mahatma Gandhi Campus, Bhavnagar 364002, Gujarat, India
关键词
antimicrobial; 2-azetidinone; catalyst; indole; beta-lactam; MIC; 1,2,3,4-tetrahydropyrimidine; BIOLOGICAL EVALUATION; INDOLE; DERIVATIVES; DISCOVERY; INHIBITORS; ANALOGS; MOIETY; POTENT;
D O I
10.1515/hc-2016-0032
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
In continuation of our work towards synthesizing bio-active molecules we developed and optimized the methodology for novel N-(3-chloro-2-oxo-4-phenylazetidin-1-yl)-4-(1H-indol-3-yl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide analogues from readily available starting materials. We focused on the pressing demand to find eco-friendly pathways by means of catalytic optimization of the process. All synthesized compounds were screened for in vitro antibacterial and antifungal activities on Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Staphylococcus pyogenes, Candida albicans, Aspergillus niger, and Aspergillus clavatus species.
引用
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页码:131 / 136
页数:6
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