3,5-Dimethyl-2,4,6-trimethoxychalcone Lessens Obesity and MAFLD in Leptin-Deficient Mice.

Chalcones constitute an important group of natural compounds abundant in fruits and comestible plants. They are a subject of increasing interest because of their biological activities, including anti-diabetic and anti-obesity effects. The simple chalcone structural scaffold can be modified at multiple sites with different chemical moieties.

Synthesis and antiprotozoal activity of original porphyrin precursors and derivatives.

Importance of heme in African trypanosomes, Leishmania sp. and Plasmodium sp. metabolisms justifies considering the potential of porphyrins and their precursors and derivatives as potential antiparasitic agents by interfering with heme metabolism.

Oxidation of antiparasitic 2-substituted quinolines using metalloporphyrin catalysts: scale-up of a biomimetic reaction for metabolite production of drug candidates.

A study comparing the chemical oxidation of drug candidates with cell-based metabolism (liver microsomes, hepatocytes) shows that biomimetic oxidation can replace the biological approach, thus allowing access to large quantities of metabolites, which can also be used for the preparation of new products.

Cross-Diels-Alder reactions of 6-oxo-1-sulfonyl-1,6-dihydropyridine-3-carboxylates.

Electron-poor 6-oxo-1-sulfonyl-1,6-dihydropyridine-3-carboxylates 1b-d undergo cross-Diels-Alder reactions with electron-rich dienes 4a-f under hyperbaric conditions, reacting either as dienophiles to yield normal-electron-demand (NED) cycloadducts 10 and/or 11 or as dienes to give inverse-electron-demand (IED) cycloadducts 12 and/or 13. The latter are converted into 14 and/or 15 through an NED cycloaddition with a second equivalent of electron-rich diene. Acyclic dienes display a propensity to yield NED products, whereas cyclic dienes tend to favor IED cycloadducts.

Synthesis and binding affinity to human alpha and beta estrogen receptors of various 7-hydroxycoumarins substituted at 4- and 3,4- positions.

The study of the relative binding affinity (RBA) to the human alpha and beta estrogen receptors (ERs) of various 7-hydroxycoumarins substituted at 4- and 3,4- positions is weak and lacks in selectivity for both ERalpha and ERbeta. The 4-(4-hydroxyphenyl)-7-hydroxycoumarin shows a weak RBA to ERbeta and 3,4-diphenyl-7-hydroxycoumarin presents a stronger RBA to ERalpha than ERbeta.