A reliable LC-MS/MS analytical method for the determination of residual triclabendazole and its principal metabolites (triclabendazole sulfoxide, triclabendazole sulfone and keto-triclabendazole) in bovine tissues was developed, in which triclabendazole and its metabolites are oxidized to keto-t...

We have reported potent peptidic and non-peptidic BACE1 inhibitors with a hydroxymethylcarbonyl (HMC) isostere as a substrate transition-state mimic. However, our potent inhibitors possess a tetrazole ring at the P1′ position. It is desirable that central nervous system (CNS) drugs do not posse...

A new carboxylic acid reductase (CAR) gene from Segniliparus rotundus DSM 44985 was overexpressed in Escherichia coli. The recombinant enzyme exhibited high activity toward a variety of aromatic and aliphatic carboxylic acids. Especially, it effectively reduced 4-hydroxybenzoic acid (8a) and 4-n...

Brevilin A is a sesquiterpene lactone isolated from Centipeda minima and possesses inhibitory effects on proliferation of various tumor cells. In this study, Brevilin A inhibitory effect on proliferation and its molecular mechanism of action were investigated both in vivo and in vitro in colon a...

The regiospecific reduction and Favorskii rearrangement of enantiopure tetrabromoepifenchone, which could be easily obtained by bromination of camphor, have been investigated. The selective formation of new functionalized chiral bicyclo[2.2.1]heptane and bicyclo[2.1.1]hexane derivatives in good ...

A new series of N-[5-(4-(alkyl/aryl)-3-nitro-phenyl)-[1,3,4-thiadiazol-2-yl]-2,2-dimethyl-propionamide 4 (a–l) and 6-(4-Methoxy-phenyl)-2-(4-alkyl/aryl)-3-nitro-phenyl)-Imidazo [2,1-b] [1,3,4] thiadiazole 6 (a–l) were synthesized starting from 5-(4-Fluoro-3-nitro-phenyl)-[1,3,4] thiadiazole-2-...

New 1,3,4-thiadiazole compounds were synthesized through the cyclization reaction of 4-phenoxybutyric acid and N-phenylthiosemicarbazide derivatives with phosphorous oxychloride. The structures of 1,3,4-thiadiazole compounds (I–XII) were clarified using spectroscopic methods such as FT-IR, 1H N...

A series of 2-substituted 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indoles was synthesized as potential antagonists for the NR1a/2B subtype of N-methyl-d-aspartate (NMDA) receptors. Assayed by electrical recording under steady-state conditions, 7-hydroxy-2-(4-phenylbutyl)-1,2,3,4-tetrahydropyrido-[3,4...

In view of coexistence of opioid and cholecystokinin (CCK) in the brain areas concerned with pain processing, some semirigid racemic and chiral analogues of a potent CCK receptor antagonist (benzotript) have been synthesized and tested for their modulatory role on opioid antinociception, which m...

BackgroundExposure to bisphenols and phthalates in pregnancy may lead to adverse health effects in women themselves and their offspring.

To assess human exposure to hazardous diesters of phthalic acid and their substitute di-iso-nonyl cyclohexane-1,2-dicarboxylate (DINCH), concentrations of their metabolites in urine should be determined. For the purpose of this biomonitoring study, a quick and easy sample preparation procedure f...

Toll-like receptors (TLRs) are promising targets for treatment of viral infections, autoimmune diseases, and cancers. Here, two new series of selective small-molecule TLR7 agonists with novel scaffolds and good selectivity over TLR8 are described, some with potencies in the low micromolar range....

The trifluoromethanethiolate anion may be generated in situ by the reaction of thiophosgene with potassium fluoride in acetonitrile. This system is used to prepare trifluoromethyl aryl sulfides from activated fluoro- and chloroaromatic substrates via nucleophilic substitution.

A new series of five thermally and dimensionally stable aromatic poly(ether-imide)s consisting of an electron donating ortho-catenated triphenylamine (TPA) derivative bearing two trifluoromethyl groups and various electron-accepting phthalimide moieties were synthesized and thoroughly investigat...

Direct dehydroxytrifluoromethylthiolation of enols and electron-deficient phenols with AgSCF3 in the presence of n-Bu4NI and KI is reported, affording a series of vinyl and aryl trifluoromethyl sulfides in moderate to excellent yields. This work represents a rare example of direct functionalizat...

Diverse of 1,2,3,9-tetrahydropyrrolo[2,1-b]quinazoline-1-carboxylic acid derivatives were designed, synthesized and evaluated for their neuroprotective activity against NMDA-induced cytotoxicity in vitro, and 5q exhibited excellent neuroprotective activity. The compound 5q was selected for furth...

The lipophilicity of 17 newly synthesized potential NMDA and cholecystokinin antagonist 2-methyl-4-oxo-3H-quinazoline-3-alkyl-carboxylic acid derivatives has been investigated. The apparent partition coefficients of two amphoteric compounds of overlapping protonation (Q1 and Q2) were determined ...

The protonation macroconstants (log K) of 4(3H)-quinazolone (1) and two 2-methyl-4-oxo-3H-alkyl-quinazoline-3-carboxylic acid derivatives (2,3) were determined by pH-potentiometry. The acid–base chemistry of compounds 2 and 3, where proton-bindings take place in an overlapping fashion, was desc...

Using the technique of cell electrophoresis to estimate surface charge density of mammalian tumor cells, a phthalanilide derivative (NSC 38280) caused a significant fall in cell electrophoretic mobility. These results suggest that the drug forms an irreversible complex with cell surface componen...

While aliphatic 2-hydroxyalkanoic acids have been more or less successfully enantioseparated with various chiral stationary phases by HPLC and GC, analogous applications on underivatized aliphatic 3-hydroxyalkanoic acids are completely absent in the scientific literature. With the aim of closing...