Synthesis and Biological Evaluation of Nitro-substituted chalcones as potent Antibacterial and Antifungal agents

Abstract

In recent years, complications of micro-organisms, which becomes drug-resistant, have extended dreadful level across the globe. One of the significant challenges in drug discovery to overcome the increased development of drug resistance is developing novel chemical moieties that advantageously comprise chemical features different from existing chemical entities. This communication presents the synthesis, docking, and antibacterial and antifungal evaluation of nitro chalcones. New series of nitro substituted chalcone derivatives (1-12) were synthesized via Claisen-Schmidt condensation using substituted acetophenone and various substituted benzaldehydes in the presence of base and ethanol. Spectral analysis of the synthesized compounds was carried out using 1H-NMR, IR, 13C-NMR and HRMS methods. Synthesized derivatives were evaluated for antimicrobial potency via the microdilution method against two Gram-positive and two Gram-negative bacterial strains and two fungal strains. All compounds showed promising antimicrobial potency. However, compound 6 was the most potent derivative of the series against all the tested antibacterial strains. Compounds 10 and 12 were found to be the most potent analogues of the series against all the tested antifungal strains. All the synthesized derivatives had good antifungal potency in comparison to the antibacterial potency. Based on the preliminary study results, the study concluded that the synthesized chalcones derivatives promise antimicrobial activity that may be further investigated to achieve antimicrobial lead.