In the present work, the characterization of the biotransformation and bioactivation pathways of the cannabinoid receptor 1 antagonist rimonabant (Acomplia) is described. Rimonabant was approved in Europe in 2006 for the treatment of obesity but was withdrawn in 2008 because of a significant drug-related risk of serious psychiatric disorders. The aim of the present work is to characterize the b...

The unexpected formation of an oxazole ring has occurred during synthesis a copper(I) cyanide network polymer as part our ongoing studies the structural chemistry these networks. Crystals title compound were formed previously reported CuCN solid containing protonated N-methylethanolamine and have been characterized by single crystal X-ray structure analysis. shows well-defined oxazole-2-iminium...

The cover picture shows the zwitterionic iminium phosphate [P(C2F5)2F3{C(NEt2)(CHF-CF3)] obtained by reaction of Ishikawa's reagent Et2N-CF2-CHF-CF3 with Lewis-acidic P(C2F5)2F. fluorinating most likely transfers a fluoride ion onto phosphorus center, transiently forming [Et2N=CF-CHF-CF3][P(C2F5)2F2]. α-fluorine atom cation [Et2N=CF-CHF-CF3]+ is labile towards substitution. Subsequently, insert...

5,10-Methenyltetrahydrofolate synthetase (MTHFS) regulates the flow of carbon through the one-carbon metabolic network, which supplies essential components for the growth and proliferation of cells. Inhibition of MTHFS in human MCF-7 breast cancer cells has been shown to arrest the growth of cells. Absence of the three-dimensional structure of human MTHFS (hMTHFS) has hampered the rational desi...

Ruthenium-catalyzed oxidative cyanation of tertiary amines with molecular oxygen in the presence of sodium cyanide and acetic acid gives the corresponding alpha-aminonitriles, which are highly useful intermediates for organic synthesis. The reaction is the first demonstration of direct sp(3) C-H bond activation alpha to nitrogen followed by carbon-carbon bond formation under aerobic oxidation c...

Quaternary benzo[c]phenanthridine alkaloids are secondary metabolites of the plant families Papaveraceae, Rutaceae, and Ranunculaceae with anti-inflammatory, antifungal, antimicrobial and anticancer activities. Their spectral changes induced by the environment could be used to understand their interaction with biomolecules as well as for analytical purposes. Spectral shifts, quantum yield and c...