Microwave-Assisted One-Pot Synthesis of Aminopyrimidine Scaffolds and their Biological Evaluation

Synthesis of aminopyrimidine derivatives was carried out by microwave synthesis. This microwave-assisted heating is an eco-friendly method. Aminopyrimidines were modified by using substituted benzaldehydes, acetophenones, and uracil during synthesis. Compounds were screened pharmacologically against the cancer cell lines. To synthesize the uracil substituted amino pyrimidines involving aldol condensation. The Invitro cytotoxicity studies against the cancer cell lines using MTT assay and the antimicrobial resistance using the bacterial and fungal strains. Aminopyrimidines were synthesized by condensation of chalcones and guanidine and further substituted with uracil. These aminopyrimidine derivatives were analyzed by FT-IR, 1H NMR, and MASS spectra. Compounds were evaluated for cytotoxicity studies against the HeLa and Vero cancer cell lines using an MTT assay. Antibacterial and antifungal activity by cup plate and two-fold serial dilution method was done. Substituted amino pyrimidines were synthesized by microwave-assisted heating and yielded in the range of 33-56%. Melting point, solubility, and spectral analysis were carried out. All the compounds exhibited no cytotoxicity. The compounds C7, C9, and C12 were viable the most at the concentration of 625µg/ml against HeLa and Vero cell lines. The compound C10 showed the highest zone of inhibition against the bacteria Mycobacterium phlei, Bacillus cereus, and Escherichia coli by both cup plate and serial dilution methods. It exhibited more inhibition against the fungi Aspergillus niger than the bacteria. The compounds with nitro substituted were found to be more effective than any other substitution. The aminopyrimidine derivatives synthesized by microwave procedure were evaluated for antimicrobial screening. It resulted in similar inhibition as ciprofloxacin. This work would serve the researchers for the eco-friendly method of synthesis and screening drugs for antimicrobial activity.