Background: Microbial infections is a global public health problem. The aim of this
work was to synthesize and evaluate the antimicrobial activity of novel triazoles, morpholines and
Methods: Compounds were synthesized using 2,4-Dihydroxyacetophenone and 4-hydroxybenzaldehyde
as starting materials. The antimicrobial activity of these compounds against bacteria
and yeast was evaluated by the broth microdilution method.
Results: The proposed route for synthesis gave high to moderate yields, moreover these compounds
were successfully characterized by 1H NMR, 13C NMR and LC-MS. Antimicrobial testing
indicated that the thiosemicarbazone and morphine derivatives had the best antimicrobial activity
against the microorganisms tested with minimum inhibitory concentrations (MIC) between 0.29
and 5.30 µM. Thiosemicarbazone derivative (12) was able to inhibit the growth of C. tropicalis,
with minimum fungicidal concentration (MFC) of 0.55 µM. In addition, this compound was active
against E. coli, S. aureus and S. epidermidis, with MIC values ranging from 0.29 to 1.11 µM.
Moreover, the morpholine derivative (15) had an MIC value of 0.83 µM against C. albicans and
Conclusion: We have efficiently synthesized a series of eleven novel triazoles, thiosemicarbazones
and morpholine derivatives using 2,4-Dihydroxyacetophenone and 4-hydroxybenzaldehyde
as starting materials. Thiosemicarbazone derivative (12) showed promising antifungal and antibacterial
activity and these findings suggest that this compound can be used as scaffolds to design
new antimicrobial drugs.