Direct Synthesis and Antimicrobial Evaluation of Structurally Complex Chalcones

Abstract

A variety of chalcone derivatives were synthesized via aldol condensation of diverse aldehydes with acyclic and cyclic ketones, under mild reaction conditions. Reaction yields of pure products fluctuated from 48 % to 81 %. An unusually wide range of substrates including quinolines, thiophenes, pyridines, and fluorinated compounds were synthesized for this study. Full characterization data, along with in vitro antimicrobial activity for all adducts, are herein reported. Whole cell growth inhibition assays against staphylococcus aureus, escherichia coli, klebsiella pneumonia, acinetobacter baumannii, pseudomonas aeruginosa, candida albicans and cryptococcus neoformans var. grubii were performed employing all synthesized compounds (3a-m).

Thiophene‐containing compounds with antimicrobial activity

“…[ 193 ] Finally, the percentage of inhibition of antibacterial and antifungal growth has been determined for a few thiophene‐containing chalcone analogs with random and diverse complex structures at a concentration of 32 μg/ml, but the obtained values were not higher than 25% for any of these compounds. [ 194 ]…”

Recent advances in chemistry and therapeutic potential of functionalized quinoline motifs – a review

“…2 Typical drug design formulations attempt to imitate naturally available heterocycles and exercise potency by disrupting and intercepting regular pathways essential for the growth of pathogenic organisms. 3 They have contributed significantly to society through their use as therapeutic agents, 4–6 application in human and veterinary medicine, 5 use in agriculture, 7,8 dyes, 9 polymers, 10 bioinformatics, 11 and molecular engineering 12 and they are of increasing importance in many other areas.…”

The Chemical and Pharmacological Advancements of Quinoline: A Mini Review

“…9 Typical drug design formulations make an effort to mimic naturally occurring heterocycles and exert potency by interfering with and interrupting the normal pathways required for the development of harmful organisms. Through their use as therapeutic agents, 10,11,12,13 applications in human and veterinary medicine, 12 use in bioinformatics, 14 agriculture, 15,16 polymers, 17 dyes, 18 and molecular engineering, 19 as well as their growing significance in numerous other fields, they have made a significant contribution to society.…”