Synthesis, characterization and antibacterial activity of (E)-chalcone derivatives

Abstract

KEYWORDS(E)-Chalcone derivatives were synthesized by the Claisen-Schmidt condensation of aromatic aldehydes with methyl ketones. 5-Arylfuran-2-carboxaldehydes (1a-b) were synthesized by Meerwein´s method and condensed with 2-acetylpyrole or 2-acetylfuran to produce the new chalcone derivatives (2a-d). The new chalcones were characterized using FT-IR and GC-MS. The synthesized compounds were also screened against some bacterial species to evaluate their activity as promising antibacterial agents.

Chalcone: A Promising Bioactive Scaffold in Medicinal Chemistry

“…The extensive analysis of bacterial studies proves that heterocyclic chalcones are superior to homocyclic chalcones. The trans -chalcone containing a difurano ring ( 103 ) (28 µM) potentially better inhibits the activity of S. aureus compared to the standard drug amoxicillin [ 144 ]. The thiazole-containing chalcone 104 (1.4 µM) is similar to vancomycin against S. aureus [ 145 ].…”

Synthesis and structural characterization of novel O-substituted phenolic and chalcone derivatives with antioxidant activity

“…The synthetic routes to the desired compounds are outlined in Schemes 1-3. Initially, 4-O-substituted phenolic derivatives 1a-c were used as the starting materials, and were prepared via two precursors 1 and 1-(3-allyl-4-hydroxyphenyl)ethanone (2). Compounds 1a-c were synthesized by a one-pot nucleophilic substitution reaction as described in the literature.…”

“…Notably, chalcones and their derivatives have been found to be associated with various biological activities. 2 Our previous research on this class of molecules indicated that many natural and synthetic chalcones exhibit a wide spectrum of biological activities, such as antimalarial, 3 antimicrobial, 4 antifungal, 5 and antitumour activity. 6,7 Recent work has explored the introduction of an alkyltriazolyl group in the chalcone skeleton at the C-4 position to afford lead compounds for the development of new therapeutic agents.…”

Synthesis of imidazo[2,1-b][1,3,4]thiadiazole–chalcones as apoptosis inducing anticancer agents

“…Chalcones represent an important class of natural products, which are intermediate precursors of all avonoid based compounds. [1][2][3][4] Chalcones are interesting simple molecules due to their varied biological activities including anti-inammatory, 5 anti-malarial, 6,7 antituberculosis, 8 anti-HIV, 9 antiproliferative, [10][11][12][13] and inhibition of several enzymes like aromatase, topoisomerase, and certain protein-tyrosine kinases like cyclin-dependent kinases. 14 They display signicant biological activities due to their potential interactions with different proteins related to cell proliferation and apoptosis.…”