Abstract: A novel series of 1-(2,4-dimethoxy-phenyl)-3-(1,3-diphenyl-1H-pyrazol-4-yl)-propenone (3) have been prepared by the Claisen-Schmidt condensation of 1-(2,4-dimethoxy-phenyl)-ethanone (1) and substituted 1,3-diphenyl-1H-pyrazole-4-carbaldehydes (2). Substituted 1,3-diphenyl-1H-pyrazole-4-carbaldehydes (2) were prepared by Vilsmeir-Haack reaction on acetophenonephenylhydrazones to offer the target compounds. The structures of the compounds were established by IR, (1)H NMR and mass spectral analysis. All the compounds were evaluated for their anti-inflammatory (TNF-alpha and IL-6 inhibitory assays), antioxidant (DPPH free radical scavenging assay) and antimicrobial activities (agar diffusion method) against some pathogenic bacteria and fungi. Of 10 compounds screened, compounds 3a, 3c and 3g exhibited promising IL-6 inhibitory (35-70% inhibition, 10 microM), free radical scavenging (25-35% DPPH activity) and antimicrobial activities (MIC 100 microg/mL and 250 microg/mL) at varied concentrations. The structure-activity relationship (SAR) and in silico drug relevant properties (HBD, HBA, PSA, cLogP, molecular weight, E(HOMO) and E(LUMO)) further confirmed that the compounds are potential lead compounds for future drug discovery study. Toxicity of the compounds was evaluated theoretically and experimentally and revealed to be nontoxic except 3d and 3j.

Abstract: After a brief overview of the general production, market value, and uses of citrus by-products, this literature review will focus on the most highly refined “pharmaceutical grade” citrus oils and antioxidants that have been derived from peels or other fruit parts. Citrus oils have been used as a part of the perfume industry and in the practice of alternative medicine for a long time, but now there is a great deal of mainstream food processing and drug industry interest in them owing to the rediscovery or confirmation of some of their beneficial properties, as well their development for entirely new applications. Their roles as antimicrobial, immunomodulatory, and cancer chemopreventive or chemotherapeutic agents appear promising.

Abstract: Chalcones are the main precursors for the biosynthesis of flavonoids and isoflavonoids. Chalcones comprise of a three carbon α, β-unsaturated carbonyl system. These are the condensation products of aromatic aldehyde with acetophenones in the presence of catalyst. They go through a variety of chemical reactions and are found beneficial in synthesis of pyrazoline, isoxazole and an assortment of heterocyclic compounds. Chalcones play pivotal role in synthesizing a range of remedial compounds. They have exhibited impressive curative efficacy for the treatment of numerous diseases. Chalcone based derivatives have gained focus since they possess simple structures and sundry pharmacological actions. A number of techniques and schemes have been reported for the synthesis of these compounds. Amongst all the stated methods, Aldol condensation and Claisen-Schmidt condensation still hold high position. Other renowned techniques include Suzuki reaction, Witting reaction, Friedel-Crafts acylation with cinnamoyl chloride, Photo-Fries rearrangement of phenyl cinnamates etc. These innovative techniques employ various catalysts and reagents including SOCl2 natural phosphate, lithium nitrate, amino grafted zeolites, zinc oxide, water, Na2CO3, PEG400, silicasulfuric acid, ZrCl4 and ionic liquid etc. The development of improved strategies for the synthesis of α, β- unsaturated carbonyl compounds is still in demand. Briefly, we have explained the methods and catalysts used in the synthesis of chalcones in a review form to provide information for the development of new-fangled processes aiming better yield, less reaction time and minimum side effects.