Rational design of chalcone and pyrazole analogues inspired by curcumin: Synthesis and biological assessment

Chalcones, an important class of bioactive compounds, have gained significant attention due to their diverse pharmacological properties. In this study, a series of novel chalcone derivatives, inspired by the curcumin pharmacophore, were synthesized and further transformed into corresponding pyrazole derivatives. The structural modifications were aimed at enhancing their biological efficacy. The synthesized compounds were evaluated for their antibacterial and antifungal activity against various microbial strains, including drug-resistant bacteria. Notably, some derivatives exhibited promising antimicrobial potential, particularly against resistant pathogens. Additionally, selected molecules were screened for topoisomerase inhibition activity, revealing potential as enzyme inhibitors. The Structure-Activity Relationship (SAR) analysis highlighted key functional groups contributing to biological potency. The findings suggest that these novel chalcone and pyrazole derivatives could serve as promising scaffolds for antimicrobial and enzyme inhibitory drug development. Further investigations on their mechanistic aspects and pharmacokinetic properties may provide valuable insights into their therapeutic potential.