Journal of medicinal chemistry, 29(5), 600-606 (1986-05-01)
The electronic properties of orthopramides, a group of selective D-2 dopamine receptor antagonists, were investigated by calculating molecular electrostatic potentials (MEP) of model compounds with the ab initio STO-3G MO method. The various substitution patterns of the aromatic ring are
The metabolism of N,N-dimethylbenzamides by phenobarbital-induced rat liver microsomes results in the formation of N-methylbenzamides and formaldehyde. The reaction proceeds via the formation of an intermediate N-hydroxymethyl-N-methylbenzamide, which, for the microsomal oxidation of N,N-dimethylbenzamide, was isolated and characterized. Confirmation of
We identified 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide 27 as a potent mGluR1 antagonist. The compound possessed excellent subtype selectivity and good PK profile in rats. It also demonstrated relatively potent antipsychotic-like effects in several animal models. Suitable for development as a PET tracer, compound
A series of N-methylbenzamide analogues (2-18) that is structurally derived from SR 48,968, a potent neurokinin-2 (NK(2)) receptor antagonist (pK(b)9.1), has been obtained using asymmetric synthesis. Isothiocyanato-N-methylbenzamide (10-12) and bromoacetamido-N-methylbenzamide derivatives (16-18) have been designed to serve as potential electrophilic
PDE10A is a recently identified phosphodiesterase with a quite remarkable localization since the protein is abundant only in brain tissue. Based on this unique localization, research has focused extensively on using PDE10A modulators as a novel therapeutic approach for dysfunction
Notre équipe de scientifiques dispose d'une expérience dans tous les secteurs de la recherche, notamment en sciences de la vie, science des matériaux, synthèse chimique, chromatographie, analyse et dans de nombreux autres domaines..