Reaction of aryl methyl ketone with isatin in the presence of a base afforded 2- arylquinoline-4-carboxylic acid (3). Reaction of diazomethane with compound 3 yielded the ester 4. Compound 5 was prepared from the reaction of N, N'-dialkylethyl (or propyl) arnine with 4. Addition of hydrazine hydrate to compound 4a gave 2- (2- pyridyl) quinoline-4-carboxylic acid hydrazide (6). Reaction of l...

Five new phenolic compounds, 4-(beta-D-glucopyranosyloxy)-3,5-dimethoxyphenyl-propanone (8), 3-[5-[(threo) 2,3-dihydro-2-(4-hydroxy-3-methoxyphenyl)-3-hydroxymethyl-7-methoxybenzofuranyl]-propanoic acid (12), 2-[4-(3-hydroxy-1-propenyl)-2,6-dimethoxyphenoxy]-3-hydroxy-3-(4-hydroxy-3,5-dimethoxyphenyl)propyl-beta-D-glucopyranoside (13), 4-[(erythro) 2,3-dihydro-3(hydroxymethyl)-5-(3-hydropropyl)...

The non-natural amino acids (R)- and (S)-2-amino-3-fluoro-2-methylpropanoic acid 5 and (R)- and (S)-3-fluoro-2-methyl-2-N-(methylamino)propanoic acid 8 were synthesized in shorter reaction sequences than in the original report starting from enantiomerically pure (S)- and (R)-alpha-methyl-serine, respectively. The reaction sequence provided the cyclic sulfamidate precursors for radiosynthesis of...

A Series of 3-Substituted phenyl 2-(3,4-dihydroxyphenyl ethyl amino)-6-substituted quinazolin-4-(3H) ones (4a-4h) have been synthesized by the reaction of 3-Substituted phenyl -2-methylbromo-6-substituted quinazolin-4-(3H) ones (3a-3h) with dopamine (3,4 dihydroxy phenyl ethyl amine). The biological screening showed that compound 4f namely 3-(2-Chloro phenyl)2-(3, 4-dihydroxyphenyl ethyl amino)...

Glutamate spillover regulates GABAergic synaptic transmission at several CNS synapses via presynaptic ionotropic and metabotropic glutamate receptors (mGluRs). We have previously demonstrated that activation of group I-III mGluRs inhibits GABAergic transmission in the midbrain periaqueductal gray (PAG), a region involved in organizing behavioral responses to threat, stress, and pain. Here, we e...

Activation and blockade of prefrontal cortical 5-hydroxytryptamine2A (5-HT2A) receptors have been linked to the action of hallucinogenic and antidepressant/antipsychotic drugs; these effects may involve modulation of glutamate release from thalamocortical afferents. Although activation of metabotropic glutamate 2 (mGlu2) receptors may suppress 5-HT-induced excitatory postsynaptic currents (EPSC...