Affiliation:
1. Department of Chemistry, Veer Narmad South Gujarat University, Surat 395007, Gujarat, India
Abstract
Background:For rapid and sustainable synthesis, microwave irradiation method is serviceable. This present study deals with the preparation of oxadiazole and pyridine bearing 1,2,3,4- tetrahydro pyrimidine derivatives by microwave irradiation.Objective:The present study aims to carry out rapid synthesis of chloro-acetamides of oxadiazoles of Biginelli product and amino cyano derivative of pyridine by microwave-assisted heating. Our efforts are focused on the introduction of chemical diversity in the molecular framework in order to synthesize pharmacologically interesting compounds.Methods::Microwave irradiation was used for the synthesis of 2-((3-cyano-4-(3,4-dichloro phenyl)- 6-(4-hydroxy-3-methoxyphenyl) pyridin-2-yl) amino)-N-(5-(substituted) -(6-methyl-2-oxo -1,2,3,4- tetrahydro pyrimidin-5-yl)-1,3,4-oxadiazol-2-yl)acetamide by using Biginelli reaction. New structural analogues were confirmed by spectral studies followed by their screening for in vitro antibacterial activity against Staphylococcus aureus, Staphylococcus Pyogenus, Escherichia coli and Pseudomonas aeruginosa bacterial strains and for antifungal activity against Candida albicans, Aspergillus niger and Aspergillus clavatus by micro-broth dilution method. In vitro antimycobacterial activity determined out against (Mycobacterium tuberculosis) H37Rv strain using Lowenstein-Jensen medium.Results:As compared to the conventional method, microwave irradiation method is advantageous for the synthesis of 1,2,3,4-tetrahydropyrimidin derivatives. Potent antimicrobial activities and antitubercular activity were found for some of the compounds.Conclusion:Microwave irradiation method provided an effective way to discover a novel class of antimicrobial and antituberculosis agents. 1,2,3,4-tetrahydropyrimidin derivatives showed improved antimicrobial and good antituberculosis activity.
Publisher
Bentham Science Publishers Ltd.
Reference30 articles.
1. Lancaster M.; Royal Society of Chemistry 2010,1-16
2. Joshi U.J.; Gokhale K.M.; Kanitkar A.P.; Green Chemistry: need of the hour. Indian J Pharm Educ Res 2011,45,168-174
3. Ravichandran S.; Karthikeyan E.; Microwave Synthesis: A potential tool for green chemistry. Int J Chemtech Res 2011,3,466-470
4. Kappe C.O.; Recent advances in the Biginelli dihydropyrimidine synthesis. New tricks from an old dog. Acc Chem Res 2000,33(12),879-888
5. Mohamed M.I.; Kandile N.G.; Zaky H.T.; Synthesis and antimicrobial activity of 1,3,4-oxadiazole-2(3h)-thione and azidomethanone derivatives based on quinoline-4-carbohydrazide derivatives. J Hetero Chem 2017,54,35-43
Cited by
12 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献