Twenty‐seven novel chalcone derivatives were synthesized using Claisen‐Schmidt condensation and their antimalarial activity against asexual blood stages of Plasmodium falciparum was determined. Antiplasmodial IC50 (half‐maximal inhibitory concentration) activity of a compound against malaria parasites in vitro provides a good first screen for identifying the antimalarial potential of the compound. The most active compound was 1‐(4‐benzimidazol‐1‐yl‐phenyl)‐3‐(2, 4‐dimethoxy‐phenyl)‐propen‐1‐one with IC50 of 1.1 μg/mL, while that of the natural phytochemical, licochalcone A is 1.43 μg/mL. The presence of methoxy groups at position 2 and 4 in chalcone derivatives appeared to be favorable for antimalarial activity as compared to other methoxy‐substituted chalcones. Furthermore, 3, 4, 5‐trimethoxy groups on chalcone derivative probably cause steric hindrance in binding to the active site of cysteine protease enzyme, explaining the relative lower inhibitory activity.

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Fluoroquinolone analogs were synthesized by reductive amination and screened for their antibacterial activities against E. coli K12 and S. aureus RN4220. Out of 18 compounds under the present study, 8 compounds were found most active against S. aureus RN4220 and E. coli K12, respectively, with MIC \ 0.062 lg/mL, which sufficiently potent for possible clinical application. All synthesized compounds were characterized by various spectroscopic techniques viz. IR, 1 H and 13 C NMR, and mass spectrometry. Out of these, one compound (3) was also characterized by the single crystal X-ray analysis. In order to understand the molecular interactions of these compounds (5-22) with enzyme DNA gyrase, molecular docking of two compounds viz. compounds 9 and 11 was also performed and we found promising results.