一些新型吡唑并[3,4-]嘧啶-4(5)-酮衍生物作为潜在抗菌剂的合成
Synthesis of some novel pyrazolo[3,4-] pyrimidin-4(5)-one derivatives as potential antimicrobial agent.
作者信息
Sureja Dipen K, Dholakia Sandip P, Vadalia Kantilal R
机构信息
Department of Pharmacy, Sumandeep Vidyapeeth, Vadodara, Gujarat, India.
Shankersinh Vaghela Bapu Institute of Pharmacy, Gandhinagar, Gujarat, India.
出版信息
J Pharm Bioallied Sci. 2016 Oct-Dec;8(4):321-326. doi: 10.4103/0975-7406.199337.
OBJECTIVES
The aim of the present work was to synthesize a novel series of pyrazolo[3,4-]pyrimidin-4(5)-one derivatives and evaluate their antimicrobial activity.
METHODS
Cyclization of an ortho-amino ester of 1-(2,4-dinitrophenyl)pyrazole with various aliphatic/aromatic nitriles under different reaction conditions such as conventional and microwave assisted synthesis, provided pyrazolo[3,4-] pyrimidin-4(5)-one derivatives. All the synthesized compounds were evaluated for their antimicrobial activity against selected bacteria and fungi by agar well diffusion method.
RESULTS
All newly synthesized compounds were characterized using spectral and elemental analysis. Compounds 2e, 2f, and 2g showed significant antimicrobial activity as compared to standard drugs used.
CONCLUSION
The newly synthesized compounds could be useful templates for the design and optimization of more active analogs as a possible antimicrobial agent.
目的
本研究的目的是合成一系列新型的吡唑并[3,4 - ]嘧啶 - 4(5)-酮衍生物，并评估它们的抗菌活性。
方法
在常规和微波辅助合成等不同反应条件下，使1-(2,4 - 二硝基苯基)吡唑的邻氨基酯与各种脂肪族/芳香族腈进行环化反应，得到吡唑并[3,4 - ]嘧啶 - 4(5)-酮衍生物。通过琼脂孔扩散法评估所有合成化合物对选定细菌和真菌的抗菌活性。
结果
所有新合成的化合物均通过光谱和元素分析进行了表征。与所用标准药物相比，化合物2e、2f和2g表现出显著的抗菌活性。
结论
新合成的化合物可能是设计和优化更具活性类似物作为潜在抗菌剂的有用模板。
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