3,4-Dihydropyrimidin-2(1H)-One Analogues: Microwave irradiated Synthesis with Antimicrobial and Antituberculosis Study

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Author(s): Dr. Navin Patel* , Sabir Pathan , Hetal I. Soni .

Journal Name: Current Microwave Chemistry

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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-tetrahydropyrimidin derivatives by microwave irradiation.

Objective: Present study aims to 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 frame work in order to synthesize pharmacologically interesting compounds.

Methods: Microwave irradiation 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. While antifungal activity against Candida albicans, Aspergillus niger and Aspergillus clavatus by micro-broth dilution method. In vitro antimycobacterial activity was carried out against (Mycobacterium tuberculosis) H37Rv strain using Lowenstein-Jensen medium.

Results: As compared to conventional method microwave irradiation method is advantageous for synthesis of 1,2,3,4-tetrahydropyrimidin derivatives. Potent antimicrobial activities and antituberculer activity found for some of the compounds.

Conclusion: Microwave irradiation method provided an effective way to discover novel class of antimicrobial and antituberculosis agents. 1,2,3,4-tetrahydropyrimidin derivatives showed improved antimicrobial and good antituberculosis activity.

Keywords: 4-Dihydropyrimidin-2(1H)-one, 4-Oxadiazole, Antimicrobial activity, Antimycobacterial activity., Microwave irradiation, Spectral studies

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(E-pub Ahead of Print)
DOI: 10.2174/2213335606666190724093305

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