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.