Design, Synthesis, Antimicrobial Screening and Docking Studies of Newer 1,4‐Dihydropyridine tethered Chalcone Hybrids

Abstract

The evolution of antimicrobial drug resistance demands the development of more effective therapeutics that are more potent with reduced side effects. In the present study, we reported the design and synthesis of 1,4-dihydropyridine clubbed with chalcone hybrids in excellent yields. Further, the biological assessment of these 1-phenyl-3-dihydropyridineprop-2-en-one chalcone hybrids as antimicrobial agents was accomplished against strains E.coli, Klebsiella pneumonia, Salmonella typhi, Staphylococcus aureus, Candida albicans (Yeast), Aspergillus niger, Alternaria solani and Fusarium oxy-sporum by well diffusion method in terms of zone of inhibition (in mm). Some Hybrids displayed the best anti-microbial activity against all the tested strains. A molecular docking study was performed for the most active compounds and showed the best binding pose with the highest binding score within the active sites of S. aureus DNA gyrase complexed with DNA and Lanosterol 14α-demethylase. These novel products evolved as promising leads for the future development of more potent anti-microbial compounds.

Antibacterial and antileishmanial activity of 1,4-dihydropyridine derivatives

“…In addition, several compounds of this class are active against bacteria [14][15][16][17] and parasites. [18][19][20] As part of our interest in exploring the antimicrobial and antiparasitic activities of natural [21][22][23] and synthetic 8,24,25 compounds, and on the basis of the previous reports on the antibacterial 17,[26][27][28] and antileishmanial [18][19][20]29 activities of 1,4-DHP derivatives (1,, in this study we have evaluated the antibacterial action of 23 synthetic 1,4-DHPs against a representative panel of cariogenic bacteria and their antileishmanial activity against L. amazonensis promastigotes.…”