The aim of this study was to synthesize three nitro substituted chalcones and to evaluate their anti-inflammatory activity in the model of carrageenan induced edema in rats. The nitro chalcone were prepared by aldol condensation using of mechanical agitation and environmentally friendly solvents with 72-73% yields in approximately 2h. The three structures were evaluated on biological activity at dose of 200mg/kg and they showed anti-inflammatory protective effect by both oral and intraperitoneal administration, this effect was time dependent.

Herein, a specialized review of the origin and state of the art of proline-derived long-aliphatic-chain amphiphilic organocatalysts (PDLACAOs) and their use in asymmetric organic reactions in aqueous media (water, brine, and sea water), including in water and in the presence of water, is presented. The reactions in which they have been evaluated and the most important mechanisms are discussed. Scheme 24. Michael addition reaction of dicyanoolefins 57 to α,β-unsaturated aldehydes 48 in-brine using catalyst 46 g, by Loh. Scheme 25. Michael addition reaction in brine using catalysts 59 a-c, by Ni and Headley. Scheme 26. Cross-aldol reaction using catalyst 59 c in the presence of ionic liquid system 64 in brine, by Ni and Headley.

We aimed to develop a standardized methodology to determine the metabolic profile of organic extracts from Malvaviscus arboreus Cav. (Malvaceae), a Mexican plant used in traditional medicine for the treatment of hypertension and other illnesses. Also, we determined the vasorelaxant activity of these extracts by ex vivo rat thoracic aorta assay. Organic extracts of stems and leaves were prepared by a comprehensive maceration process. The vasorelaxant activity was determined by measuring the relaxant capability of the extract to decrease a contraction induced by noradrenaline (0.1 μM). The hexane extract induced a significant vasorelaxant effect in a concentration‐ and endothelium‐dependent manner. Secondary metabolites, such as polyunsaturated fatty acids, terpenes and one flavonoid, were annotated by liquid chromatography/quadrupole time‐of‐flight mass spectrometry (LC/QTOF‐MS) in positive ion mode. This exploratory study allowed us to identify bioactive secondary metabolites from Malvaviscus arboreus, as well as identify potentially‐new vasorelaxant molecules and scaffolds for drug discovery.

In this article, a one‐pot methodology for the synthesis of flavanones “on‐water” from simple starting materials is reported. The reaction proceeds in basic media (KOH), at room‐temperature and in distilled water, during a period of 48 h with up to 96 % yields. In addition, most flavanones are obtained pure enough after a simple filtration procedure.

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Three functionalized chalcones containing combinations of nitro functional groups have been synthesized via Claisen-Schmidt condensation between 2-nitroacetophenone and nitrobenzaldehyde, and the crystal structures obtained ((E)-1,3-bis(2-nitrophenyl)prop-2-en-1-one, 1a, (E)-1-(2-nitrophenyl)-3-(3-nitrophenyl)prop-2-en-1-one, 1b and (E)-1-(2-nitrophenyl)-3-(4-nitrophenyl)prop-2-en-1-one, 1c), C15H10N2O5, are reported. Compounds 1a and 1c crystallized in the triclinic centrosymmetric space group P1¯, whereas compound 1b crystallized in the orthorhombic space group Pbca. The X-ray analysis reveals that structures 1a and 1b exhibits s-trans conformation, whereas structure 1c exists in s-cis conformation, concerning the olefinic double bonds. In addition, the results show that the position of the nitro substituent attached to the aromatic B-ring has a direct effect on the molecular coplanarity of these compounds. The Hirshfeld surface analysis suggests that the non-covalent π-π stacking interactions are the most important contributors for the crystal packing of 1a and 1b. In 1c, the crystal packing is mainly stabilized by weak intermolecular C―H···O interactions due to the planar nature of the molecule.

Synthesis and Antiinflammatory Activity of Three Nitro Chalcones. -The three new compounds (III) show antiinflammatory protective, time dependent effect by both oral and intraperitoneal administration. Compound (IIa) is found to be the most effective, one with no statistically significant difference when compared to reference drug (meloxicam). -(GOMEZ-RIVERA, A.; AGUILAR-MARISCAL, H.; ROMERO-CERONIO, N.; ROA-DE LA FUENTE, L. F.; LOBATO-GARCIA*, C. E.; Bioorg. Med. Chem. Lett. 23 (2013) 20, 5519-5522, http://dx.doi.org/10.1016/j.bmcl.2013.08.061 ; Div. Acad. Cienc. Basicas, 86690 Tabasco, Mex.; Eng.) -C. Cyrus

A simple and efficient one-pot, three-component synthetic method for the preparation of coumarin-3-carboxamides was carried out by the reaction of salicylaldehyde, aliphatic primary/secondary amines, and diethylmalonate. The protocol employs piperidine-iodine as a dual system catalyst and ethanol, a green solvent. The main advantages of this approach are that it is a metal-free and clean reaction, has low catalyst loading, and requires no tedious workup.