Synthesis and biological evaluation of anti-inflammatory activity of 1,3 diphenyl propenone derivatives

Abstract

A series of five chalcone derivatives were synthesized by Claisen-Schmidt condensation of acetophenone with appropriately substituted benzaldehyde in the presence of aqueous alkali. The synthesized compounds were characterized by their IR, NMR, and Mass spectral data. These compounds have been subjected to anti-inflammatory screening using the carrageenan-induced rat hind paw edema model. Chalcone derivatives at dose 25 mg/kg by oral route inhibited significantly the formation of edema. Chalcone posses a highly electrophilic a,b-unsaturated carbonyl moiety showed better anti-inflammatory activity.

Ferrocenyl chalcones with O-alkylated vanillins: synthesis, spectral characterization, microbiological evaluation, and single-crystal X-ray analysis

“…Chalcones (1,3-diaryl-2propen-1-ones) and their derivatives exhibit different pharmacological and biological activities, the major ones being antifungal (Bag et al, 2009;Lahtchev et al, 2008;Mostahar et al, 2007), antimicrobial (Yayli et al, 2006;Trivedi et al, 2008;Opletalova, 2000;Katade et al, 2008), anticonvulsant (Kaushik et al, 2010), antioxidant (Vasilev et al, 2010Vogel et al, 2008, Cheng et al, 2008, antiprotozoal (Lunardi et al, 2003), antitrichomonal (Oyedapo et al, 2004), antimalarial (Motta et al, 2006;Awasthi et al, 2009;Lim et al, 2007;Wu et al, 2002;Liu et al, 2001), anti-inflammatory (Yadav et al, 2010;Zhang et al, 2010;Herencia et al, 1998;Nowakowska 2007), trypsin inhibition (Maliar et al, 2004) and anti-cancer activity (Achanta et al, 2006;Romagnoli et al, 2008;Echeverria et al, 2009;Szliszka et al, 2009;Ilango et al, 2010;Wattenberg et al, 1994;Edwards et al, 1988;Kumar et al, 2011;Seo et al, 2010). Chalcones (1,3-diaryl-2propen-1-ones) and their derivatives exhibit different pharmacological and biological activities, the major ones being antifungal (Bag et al, 2009;Lahtchev et al, 2008;Mostahar et al, 2007), antimicrobial (Yayli et al, 2006;…”

Chalcones, semicarbazones and pyrazolines as inhibitors of cathepsins B, H and L

“…Chalcones, another class of biologically active molecules, known to possess antimalarial [9], anticancer [10], antiprotozoal [11], anti-inflammatory [12], antibacterial [13], antioxidant [14], antifungal [15] activities are also reported to inhibit various enzymes like tyrosinase, alpha-amylase and beta-lectamase [16][17][18]. These, ␣,␤-unsaturated compounds have been found to interact with serum albumin [19][20][21][22][23][24], the protein responsible for the transportation of various molecules including drugs.…”

Synthesis of some dihydropyrimidine-based compounds bearing pyrazoline moiety and evaluation of their antiproliferative activity

“…Compounds 4a, 4c, 4f, 4g [24], 4b [25], 4d, 4e [26] and 4h [27] were synthesized according to the literature procedures.…”