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Microwave assisted synthesis and antimicrobial evaluation of novel substituted thiosemicarbazide derivatives of pyrimidine
Journal of Heterocyclic Chemistry ( IF 2.4 ) Pub Date : 2020-06-16 , DOI: 10.1002/jhet.4013
Theivendren Panneerselvam 1 , Jithendar Reddy Mandhadi 2
Affiliation  

A new series of antimicrobial thiosemicarbazide substituted pyrimidine derivatives were synthesized by using thiosemicarbazide and ethyl 2‐((2‐amino‐5‐carbamoyl‐6‐[substituted benzyl] pyrimidin‐4‐yl)oxy)acetate derivatives and subsequent addition of acetaldehyde and acetone. The designed compounds were screened for Antibacterial activity against Staphylococcus aureus , Staphylococcus epidermidis , Micrococcus luteus , Bacillus cereus , Escherichia coli , Pseudomonas aeruginosa , and Klebsiella pneumonia in comparison with the standard drugs Ciprofloxacin and antifungal effect against Aspergillus niger and Aspergillus fumigates in comparison with the standard drug Ketoconazole reveal the potency of synthesized derivatives. In accordance with the data obtained from antimicrobial activity, all the synthesized derivatives have shown good activity against the tested microbes. Among them, compound bearing 2‐hydroxy and 3‐chloro derivatives of thiosemicarbazide substituted pyrimidine has shown good activity against all the tested organisms.

中文翻译:

新型嘧啶取代的硫代氨基脲衍生物的微波辅助合成及抗菌性能评价

通过使用硫代氨基脲和2-((2-氨基-5-氨基甲酰基-6- [取代的苄基]嘧啶-4-4-基)氧基]乙酸乙酯衍生物并随后加入乙醛和乙醛合成了一系列新的抗菌剂硫代氨基脲取代的嘧啶衍生物丙酮。所设计的化合物进行了筛选针对抗菌活性金黄色葡萄球菌表皮葡萄球菌藤黄微球菌蜡状芽孢杆菌大肠杆菌铜绿假单胞菌,和肺炎克雷伯氏菌与标准药物环丙沙星和针对抗真菌作用比较黑曲霉与标准药物酮康唑相比,熏蒸曲霉菌显示出合成衍生物的效力。根据从抗菌活性获得的数据,所有合成的衍生物均显示出对被测微生物的良好活性。其中,带有巯基氨基脲取代的嘧啶的2-羟基和3-氯衍生物的化合物对所有受测生物均显示出良好的活性。
更新日期:2020-08-08
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