Significance of Microwave Irradiation in Synthesis of Thiazolidin-4-one Bearing Pyrimidine Analogues: Their in vitro Antimicrobial, Antituberculosis and Antimalarial Studies

Aims: To synthesise biologically active thiazolidin-4-one by microwave irradiation method and evaluate against different species of bacteria, fungi and Plasmodium falciparum. Background: Microwave irradiation method is serviceable for rapid and sustainable synthesis. In this present study, Thiazolidin-4-one bearing pyrimidine derivatives have been synthesized by microwave irradiation method. Objective: Thiazolidin-4-one is a valuable motif because of its broad-spectrum biological evaluation. It is famous for many types of biological profiles, mainly antimicrobial, anti-tuberculosis, anti-convulsant, antihypertensive, hypoglycemic agent and antimalarial. This biological response leads our attention towards the change of Thiazolidin-4-one skeleton to enhance potential. Present study aims to carry out a rapid synthesis of Thiazolidin-4-one derivative of pyrimidine by microwave-assisted heating. Methods: 4-(4-substituted phenyl)-6-(substituted aryl) pyrimidin-2-amine was the key intermediate required for the synthesis of 3-(4-(Substituted phenyl)-6-(substituted aryl) pyrimidin-2-yl)-2-(4-hydroxy phenyl) thiozolidin-4-one (5(A-J)), which was prepared by using microwave irradiation. The structures of all newly synthesized motifs were characterized by spectral analysis (IR, H-1 NMR, C-13 NMR spectroscopy) and screened for antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Streptococcus pyogenes; antifungal activity against Candida albicans, Aspergillus niger, Aspergillus Clavatus; anti-tuberculosis activity against M. tuberculosis H37RV and antimalarial activity against Plasmodium falciparum. Results: Higher yield with less time-consuming method is the main advantage of Thiazolidin- 4-one bearing pyrimidine motifs synthesis. The excellent biological response of compounds 5(B), 5(C), 5(D), 5(G), 5(H), 5(I), and 5(J) was observed. Conclusion: As compared to conventional method, less time is required for the preparation of Thiazolidin- 4-one analogues by using advantageous microwave irradiation method. Thiazolidin-4-one derivatives showed improved biological activity.