N-Substituted amides of endo-3-(3-methylthio-1,2,4-triazol-5-yl)bicyclo[2.2.1]hept-5-ene-2-carboxylic acid and 1-(5-methylthio-1,2,4-triazol-3-yl)cyclohexane-2-carboxylic acid were prepared by the condensation reaction of endo-S-methyl-N1-(bicyclo[2.2.1]hept-5-ene-2,3-dicarbonyl)isothiosemicarbazide and S-methyl-N1-(cyclohexane-2,3-dicarbonyl)isothiosemicarbazide with primary amines. The synthe...

Changes in the expression of metabotropic glutamate receptor 5 (mGluR5) in the rat hippocampus in an animal model of depression. The aim of our study was to investigate the level of metabotropic glutamate receptors (mGluRs) in the brains of rats after chronic mild stress. Using Western blotting procedure we showed that the level of mGluR5 receptor protein was increased in CA1 and decreased in C...

Precursors of podophyllotoxin were synthesized and screened for their antibacterial activity. The results proved that ethyl-2-(3'-methyl-4'-methoxybenzoyl)-3-(4″ methoxyphenol)-cyclopropane-1-carboxylic acid and Ethyl-2-(3'-methyl-4'-methoxybenzyol-3-1 3″, 4″-dimethoxyphenyl)-cyclopropane-carboxylic acid have significant antibacterial activity against Citrobacter sp., Escherchia coli, Klebsiell...

Adathodai kudineer (AK) a Classical Siddha formulation is used to treat various fevers which cause moderate severe acute respiratory symptoms as indicated in the text. GC-MS analysis was carried out identify presence of potent lead molecules AK against novel corona virus. The aqueous extract has shown following bioactive compounds such Napthalene, Benzene Propanol, Acetic Acid, Furazan-3-amine,...

The interface of planar TiO(2)/polymer photovoltaic cells was modified with two carboxylated polythiophenes having different densities of carboxylic acid groups. Both of the interface modifiers increase the photocurrent of the cells but lower the open-circuit voltage. The work function of the TiO(2), measured using a Kelvin probe, increases with increasing density of carboxylic acid groups due ...

Free fatty acid receptor 2 (FFA2; GPR43) is a G protein-coupled seven-transmembrane receptor for short-chain fatty acids (SCFAs) that is implicated in inflammatory and metabolic disorders. The SCFA propionate has close to optimal ligand efficiency for FFA2 and can hence be considered as highly potent given its size. Propionate, however, does not discriminate between FFA2 and the closely related...

The resolved X-ray crystal structures of the glutamate-binding domain (S1/S2 domains) of the GluR2 and NR1 glutamate receptor subunits were used to model the homologous regions of the N-methyl-D-aspartate (NMDA) receptor's NR2 subunits. To test the predictive value of these models, all four stereoisomers of the antagonist 1-(phenanthren-2-carbonyl) piperazine-2,3-dicarboxylic acid (PPDA) were d...

The replacement of a carboxylic acid with a surrogate structure, or (bio)-isostere, is a classical strategy in medicinal chemistry. The general underlying principle is that by maintaining the features of the carboxylic acid critical for biological activity, but appropriately modifying the physicochemical properties, improved analogs may result. In this context, a systematic assessment of the ph...

Structure-activity relationship studies of valproic acid (VPA) derivatives have revealed a quantitative correlation between histone deacetylase (HDAC) inhibition and induction of neural tube defects (NTDs) in the NMRI-exencephaly-mouse model, but this correlation has been, so far, limited to congeners with a carboxylic acid function. Whereas the classical HDAC inhibitor trichostatin A is active...