Background: The past decade has witnessed a significant increase in the prevalence of
resistance to antibacterial and antifungal agents. To overcome this problem it is desirable to devote
continuing effort in evaluating new series of chemical entities for the identification of new antimicrobial
Methods: The alkynyl substituted 2-amino-1,4-dihydropyrimidine framework has been explored
for the identification of potential antimicrobial / cytotoxic agents. Compounds derived from this
framework were synthesized using a multi-step method involving the Biginelli reaction, followed
by chlorination and subsequent displacement of the chloro group by various amines and finally
alkynylation via a Cu-free Sonogashira coupling.
Results: Several of these compounds showed promising antimicrobial / antifungal activities and
cytotoxicity against cancer cell lines indicating their potential in reducing the danger of bacterial
infections in the immunocompromised cancer patients.
Conclusion: We have shown that the current framework could be an attractive template for the
design and generation of diversity based library of small molecules leading.