Synthesis and Biological Evaluation of Chalcone Derivatives (Mini Review)

Abstract

Chalcones are the principal precursors for the biosynthesis of flavonoids and isoflavonoids. A three carbon α, β-unsaturated carbonyl system constitutes chalcones. Chalcones are the condensation products of aromatic aldehyde with acetophenones in attendance of catalyst. They go through an assortment of chemical reactions and are found advantageous in synthesis of pyrazoline, isoxazole and a variety of heterocyclic compounds. In synthesizing a range of therapeutic compounds, chalcones impart key role. They have showed worth mentioning therapeutic efficacy for the treatment of various diseases. Chalcone based derivatives have gained heed since they own simple structures, and diverse pharmacological actions. A lot of methods and schemes have been reported for the synthesis of these compounds. Amongst all, Aldol condensation and Claisen-Schmidt condensation still grasp high up position. Other distinguished techniques include Suzuki reaction, Witting reaction, Friedel-Crafts acylation with cinnamoyl chloride, Photo-Fries rearrangement of phenyl cinnamates etc. These inventive techniques utilize various catalysts and reagents including SOCl(2) natural phosphate, lithium nitrate, amino grafted zeolites, zinc oxide, water, Na(2)CO(3), PEG400, silicasulfuric acid, ZrCl(4) and ionic liquid etc. The development of better techniques for the synthesis of α, β- unsaturated carbonyl compounds is still in high demand. In brief, we have explained the methods and catalysts used in the synthesis of chalcones along with their biological activities in a review form to provide information for the development of new-fangled processes targeting better yield, less reaction time and least side effects with utmost pharmacological properties.

Palladium‐Catalysed Cross‐Coupling Reactions for the Synthesis of Chalcones

“…In general, the synthesis of chalcone can be easily accomplished via Claisen‐Schmidt condensation reaction by mixing a benzaldehyde with an active acetophenone under either strong basic or acidic condition . It is noteworthy to mention that other uncommon reactions such as the Friedel‐Crafts alkylation, Knoevenagel condensation, and Julia‐Kocienski have also been explored and studied.…”

Highlights on the synthesis of novel phenothiazine‐based azines scaffold as antioxidant agents

“…Phenothiazine derivatives have attracted particular attention due to their therapeutic importance because they have shown a wide range of biological activities . Moreover, it is clear from the literature that the chalcone (1,3‐diphenylpropenone) fraction is a scaffolding prevalent in a number of synthetic and natural molecules with attractive potent biological activities such as antitumor, antiparasitic, antioxidant, and anti‐inflammatory activities . Recent studies reveal that chalcone analogs inhibit nitric oxide (NO, is a free radical have electron unpaired), NO‐synthetase (iNOS), and cyclooxygenase‐2 (COX‐2)‐active protein expression in cells stimulated by lipopolysaccharides (LPS), indicating the highest anti‐inflammatory activity of chalcones .…”

Studies of synthetic chalcone derivatives as potential inhibitors of secretory phospholipase A2, cyclooxygenases, lipoxygenase and pro-inflammatory cytokines

“…Chalcones belong to the group of chemical compounds that are linked to various pharmacological activities. Recently, we summarized the biological properties of chalcones 27,28. Previous reports have also demonstrated the anti-inflammatory activity of chalcone derivatives by the modulation of pro-inflammatory gene expression of COX-2, inducible nitric oxide synthase, and numerous essential cytokines 29–32.…”