40775-90-4Relevant academic research and scientific papers
Synthesis and antibacterial evaluation of thiouracil derivatives containing 1,2,4-triazolo[1,5-a]pyrimidine
Cui, Penglei,Zhang, Di,Guo, Xiumin,Ji, Shujing,Jiang, Qingmei
, p. 555 - 560 (2021/07/25)
A series of new thiouracil compounds containing 1,2,4-triazolo[1,5-a]pyrimidine were designed and synthesized. The in vitro antibacterial activities of the new compounds against Bacillus am-yloliquefaciens, Staphylococcus aureus and Bacillus subtilis were tested. The results showed that some of the new compounds had strong inhibitory activities against the tested bacteria. At the concentration of 50 μg/mL, the compound 12d had broad and the highest inhibitory activity with the 100% inhibition against the three tested strains, the same as norfloxacin which was used as the control.
Thiouracil-containing 1,2,4-triazolo[1,5-a]pyrimidine compound, and preparation method and application thereof
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Paragraph 0012-0013, (2020/08/30)
The invention discloses a thiouracil-containing 1,2,4-triazolo[1,5-a]pyrimidine compound. A preparation method for the thiouracil-containing 1,2,4-triazolo[1,5-a]pyrimidine compound comprises the following steps: with 3-amino-1,2,4-triazole, aromatic amine and an aromatic aldehyde compound as initial raw materials, dissolving 3-amino-1,2,4-triazole and ethyl 4-chloroacetoacetate in glacial aceticacid for a reflux reaction to obtain an intermediate I; further reacting the intermediate with phosphorus oxychloride and aromatic amine to obtain an intermediate II; subjecting aromatic aldehyde, ethyl cyanoacetate and thiourea to a reaction under the catalysis of piperidine to obtain an intermediate III; and reacting the intermediate II with the intermediate III in an acetonitrile solvent underthe catalysis of potassium carbonate to obtain a target product. The method provided by the invention is simple in process, easy to operate and easy for large-scale production, and experiments prove that the prepared target compound has strong bacteriostatic activity and can be widely applied to bacteriostatic pharmaceutical preparations.
