The effects of antipsychotic drugs (APDs) on the adolescent brain are poorly understood despite a dramatic increase in prescription of these drugs in adolescents over the past twenty years. Neuronal systems continue to be remodeled during adolescence. Therefore, when given in adolescence, antips...

The objective of the present study was to determine whether an in vitro-in vivo correlation (IVIVC) can be established for polymeric microspheres that are equivalent in formulation composition but prepared with different manufacturing processes. Risperidone was chosen as a model therapeutic and ...

Alzheimer’s disease (AD) is a complex neurodegenerative disorder with cognitive impairment and major neuropathologic hallmark of amyloid-beta (Aβ) peptides. Risperidone, an atypical antipsychotic, can improve concentration and cognitive deficit in schizophrenia patients. In this study, behavio...

Antipsychotic agents have been reported to promote hippocampal neurogenesis and improve cognitive deficits; yet, the molecular mechanisms underlying these actions remain unclear. In the present study, we used a murine model of schizophrenia induced by 5-day intraperitoneal injection with the non...

Inflammation and oxidative stress (IOS) are considered key pathophysiological elements in the development of mental disorders. Recent studies demonstrated that the antipsychotic risperidone elicits an antiinflammatory effect in the brain. We administered risperidone for 2-weeks at adolescence to...

Despite substantial increases in the use of antipsychotics to treat various psychiatric conditions in children, there is a lack of literature regarding long-term effects of early treatment. Some studies have indicated that early administration results in differential alterations to neurotransmis...

Estrogen-related receptor gamma (ERRγ) has recently been recognized as an attractive target for treating inflammation, cancer, and metabolic disorders. Herein, we discovered and demonstrated the in vitro pharmacology as well as the absorption, distribution, metabolism, excretion, and toxicity (...

A series of new isothiocoumarin-3-carboxylic acids derivatives had been obtained based on the 5-arylidenerhodanines hydrolysis. Anticancer activity screening allowed identification of 7,8-dimethoxy-1-oxo-1H-isothiochromene-3-carboxylic acid (4-phenylthiazol-2-yl)-amide (30) with the highest leve...

It is still unclear whether the inhibitory effect of organic acid on polyphenoloxidase (PPO) is due to the reversible inhibition or decrease of pH. In this study, cinnamic acid, citric acid and malic acid inhibited PPO in different modes. Results showed that the inhibition by cinnamic acid resul...

An expeditious and concise synthesis of highly congested 2-amino-3-aminomethyl-5-methylsulfanyl/-sec-aminobiphenyl-4-carbonitrile 4 and 1-tert-butoxycarbonyl-6-sec-amino-8-aryl-5-cyano-2-oxo-1,2,3,4-tetrahydroquinazoline 5 has been delineated through base catalyzed ring transformation of 6-aryl-...

Exclusive formation of either 2- or 4-trifluoromethyl(1H,5)arylodiazepines (5,7)(6,8) was observed in the condensation of 1,1,1-trifluoro-3-(isobutoxymethylene)-2-propanones 23 with o-arylenediamines 4 under microwave irradiation conditions. Thermal reactions under the same temperature and time ...

Exclusive formation of either 2- or 4-trifluoromethyl(1H,5)arylodiazepines 43 was observed in the condensation of 1,1,1-trifluoro-3-(isobutoxymethylene)-2-propanones (RH,COCF3) 2 with o-arylenediamines 1 under microwave irradiation conditions. Thermal reactions under the same temperature and t...

An efficient synthesis of 3-aryl-3-hydroxy-2-(1H-indol-3-yl)-1-phenyl-1-propanone via the cleavage of epoxides with indole promoted by ultrasound irradiation was carried out in good yields by using montmorillonite K10-ZnCl2 within 2–5 h at room temperature. This method provides several advantag...

(R)-1-fluoro-3-[(4-methylphenyl)sulfinyl]-2-propanone (1) reacts with diazomethane affording (S)-2-(fluoromethyl)-2-[(R)-(4-methylphenyl)sulfinyl]methyl oxirane (2) as the main product. The influence of reaction conditions (solvent, temperature) on the chemo-and stereoselectivity has been studie...

A synthesis of 3-formyl-4-pyrones by Vilsmeier-Haack reaction of substituted benzyl methyl ketones has been reported. The reaction of benzyl ethyl ketone with chloromethyleneiminium salt gave corresponding 4-pyrone while phenoxy acetone gave N,N-dimethylamino substituted pentadienaldehyde.

A simple route to 1-R-3-(2-indolyl)-1-propanones has been elaborated based on recyclization of 2-(2-aminobenzyl)furan derivatives. Being a modification of the Reissert indole synthesis, our approach employs the furan ring as a source of carbonyl function. This approach is general and allows vary...

A synthesis of 3-(pyridin-2-yl)dihydro-1,2,4-triazinone (1) is achieved utilizing the appropriate “in situ generated” nitrile imine 1,3-dipole. In solution, compound 1 rapidly reacts with dichlorobis(benzonitrile)palladium(II) to form dichloro[3-(pyridin-2-yl)dihydro-1,2,4-triazinone]palladium...

Treatment of 1-diazo-3-(2-thienyl)-2-propanone with catalytic rhodium (II) acetate results in cyclopropanation followed by acid-catalyzed ring opening and tautomerization to yield 5,6-dihydro-4H-cyclopenta[b]thiopen-5-one. Under the same conditions, however, the isomeric 1-diazo-3-(3-thienyl)-2-...

The crystal structure of the organic compound 1-(naphthylamino)-1-(p-chlorophenylhydrazono-2-propanone, 1a, comprises two crystallographically nonequivalent independent molecules in the asymmetric unit with dispositions and relative orientations amenable to inter- and intramolecular hydrogen bon...

Tris(2,4,6-trichlorophenyl)carbenium hexachloro-antimonate (2), (2,6-dichloro-4-hydroxyphenyl)bis(2,4,6-trichlorophenyl)methyl radical (4) and its methyl ether derivative 5 have been synthesized and isolated as crystalline solids. In contrast to 5, radical 4 is not very stable in air, and the di...