Alcohol provokes different molecular pathways contributing to a clinically significant neurotoxicity in different brain areas. Affected cognition in alcoholics can influence both daily life functioning and alcohol craving management abilities. Preventing alcohol-induced neurotoxicity with different neuroprotective pharmacological interventions is receiving strong scientific backgrounds from pub...

There is increasing evidence that a proton-coupled organic cation (H+/OC) antiporter facilitates uptake of various central nervous system-active drugs, such as the histamine H1 receptor antagonist diphenhydramine, into brain. The purpose this study was to clarify structural requirements for H+/OC antiporter-mediated hCMEC/D3 cells, an established in vitro model human blood-brain barrier, by usi...

This communication describes the chemoselective metal-free reduction of tertiary amides to the corresponding amines. Hantzsch ester is used as a mild reducing agent for the reduction of trifluoromethanesulfonic anhydride activated amides providing the tertiary amines with high functional group tolerance.

A direct asymmetric hydrogenation of unprotected enamino esters and amides is described. Catalyzed by Rh complexes with Josiphos-type chiral ligands, this method gives beta-amino esters and amides in high yield and high ee (93-97% ee). No acyl protection/deprotection is required.

a highly efficient procedure for the preparation of n,n'-alkylidenebisamides in the presence of bf3.sio2 as a catalyst is described. n,n'-alkylidenebisamides have been prepared via one-pot three-component condensation reaction of various aldehydes and amides. all of the reactions proceeded in high yields and in moderately short reaction times.

Allyl amides were synthesised from the reaction of allyl alcohols and halogenated nitriles using a platinum multifaceted catalysis approach in which both the nucleophilic addition and subsequent [3,3]-sigmatropic rearrangement steps of the process were catalysed by the same complex. Additionally, (1)H/(13)C{(1)H} NMR and GC studies provided the first insights into the mechanism of this transfor...

Using a simple copper catalyst, the alkylation of nitroalkanes with α-bromocarbonyls is now possible. This method provides a general, functional group tolerant route to β-nitrocarbonyl compounds, including nitro amides, esters, ketones, and aldehydes. The highly sterically dense, functional group rich products from these reactions can be readily elaborated into a range of complex nitrogen-conta...

The heteroleptic calcium amides [{ArNC(Me)CHC(Me)NAr}Ca(NR(2))(THF)] (Ar=2,6-di-iso-propylphenyl, R=SiMe(3), Ph) and the homoleptic heavier alkaline earth amides, [M{N(SiMe(3))(2)}(2)] (M=Ca, Sr and Ba) are reported as pre-catalysts for the hydroamination of isocyanates.

The arylation of secondary acyclic amides has been achieved with diaryliodonium salts under mild and metal-free conditions. The methodology has a wide scope, allows synthesis of tertiary amides with highly congested aryl moieties, and avoids the regioselectivity problems observed in reactions with (diacetoxyiodo)benzene.