Analysis of the roles of the short chain fatty acid receptor, free fatty acid 3 receptor (FFA3), has been severely limited by the low potency of its endogenous ligands, the crossover of function of these on the closely related free fatty acid 2 receptor, and a dearth of FFA3-selective synthetic ligands. From a series of hexahydroquinolone-3-carboxamides, we demonstrate that 4-(furan-2-yl)-2-met...

Analysis of the roles of the short chain fatty acid receptor, free fatty acid 3 receptor (FFA3), has been severely limited by the low potency of its endogenous ligands, the crossover of function of these on the closely related free fatty acid 2 receptor, and a dearth of FFA3-selective synthetic ligands. From a series of hexahydroquinolone-3-carboxamides, we demonstrate that 4-(furan-2-yl)-2-met...

Unripe grape juice (verjuice) as a natural catalyst was successfully applied to perform the one-pot reaction of aryl aldehydes, malononitrile, hydrazine hydrate and ethyl acetoacetate to synthesize pyranopyrazole derivatives in aqueous ethanol at room temperature in excellent yields. Furthermore, unripe grape juice catalyzed one-pot synthesis of hexahydroquinoline-3-carboxamide derivatives by t...

Despite more than 25 years of research, the molecular targets of quinoline-3-carboxamides have been elusive although these compounds are currently in Phase II and III development for treatment of autoimmune/inflammatory diseases in humans. Using photoaffinity cross-linking of a radioactively labelled quinoline-3-carboxamide compound, we could determine a direct association between human S100A9 ...

Objectives . A key step in the synthesis of natural nucleoside analogs is formation a glycosidic bond between carbohydrate fragment and heterocyclic base. Glycosylation methods differ terms regio- stereoselectivity. promising method for highly specific new pharmacologically active compounds involves an enzymatic reaction catalyzed by genetically engineered phosphorylases. This study devoted to ...

A series of new hexahydroquinoline and 1,4-dihydropyrimidine derivatives were synthesized. Condensation of 2-methyl- thiazole-4-carboxaldehyde (1) with 1,3-cyclohexanedione and alkyl 3- aminocrotonate afforded 4-(2-methyl-thiazol-4-yl)-hexahydroquinoline while condensation of aldehyde (1) with benzoyl acetone and thiourea gave 1,4-dihydropyrimidine derivatives. The stereochemistry of 1,4-dihydr...

The divergent behaviour of 3-alkynylindole-2-carboxamides, under palladium catalysed conditions and phase-transfer catalytic conditions, is described. Thus, palladium catalysed intramolecular C-N and C-C bond formation in a single step by C-H activation involving 3-alkynylindole-2-carboxamides and leading to pyrrolodiindolones in high yields is developed. In contrast, using the same precursors,...