A library-friendly approach to generate new scaffolds is decisive for the development of molecular probes, drug like molecules and preclinical entities. Here, we present the design and synthesis of novel heterocycles with spiro-2,6-dioxopiperazine and spiro-2,6-pyrazine scaffolds through a three...
We report the synthesis of novel 2-azabicyclo[3.1.1]heptane-5-carboxylic acid.
High-performance liquid chromatographic (HPLC) separation of stereoisomeric cyclic β-substituted α-quaternary α-amino acids was performed by ligand-exchange on a copper(II)-d-penicillamine chiral stationary phase. The investigated amino acids are the 1-amino-2-methylcyclohexanecarboxylic acid...
High-performance liquid chromatographic (HPLC) separation of stereomeric cyclic β-substituted α-quaternary α-amino acids was performed on a chiral stationary phase based on the glycopeptide antibiotic teicoplanin. The investigated amino acids are the 1-amino-2-methylcyclohexanecarboxylic acid...
A novel synthesis of 5-chloroalkyl-2-oxazolidinones from cyclic ethers was demonstrated. Utilizing 5- and 6-membered cyclic ethers as examples, the α-methylaminomethylcyclic ethers were cyclized to 5-(3-chloropropyl)- and 5-(4-chlorobutyl)-3-methyl-2-oxazolidinone, respectively. Several derivat...
The miscibility behaviour of poly(3-chloropropyl methacrylate) (PCPMA) and poly(2-iodoethyl methacrylate) (PIEMA) with a series of aliphatic polyesters was investigated by differential scanning calorimetry. Binary blends of PCPMA and PIEMA with poly(butylene adipate), poly(2,2-dimethyl-1,3-propy...
A novel organic–inorganic hybrid heterogeneous catalyst system was obtained from the reaction of the molybdenum(VI) complex of salicylidene 2-picoloyl hydrazone with mesoporous silica containing 3-chloropropyl groups prepared by a direct synthetic approach involving hydrolysis and co-condensati...
Organophosphate flame retardants (OPFRs) are widely used as flame retardants which are ubiquitous in various environment media. As many of OPFRs are toxic and persistent, concerns have been raised in regards to their environmental impact. In this study, the toxicological effects of tris(2-chloro...
Two diene metabolites of valproic acid (VPA),(E)-2-n-propyl-2, 4-pentadienoic acid (1) and(E)-2-(1′-propenyl)-(E)-2-pentenoic acid (2), were stereoselectively synthesized. Mesylate elimination in the final step to produce the unsaturation at position 2 was stereospecific for the(E)-configuratio...
An improved method for the quantitative determination of valproic acid (VPA) and sixteen of its metabolites has been developed using gas chromatography-mass spectrometry with selected-ion monitoring. The method is applicable to serum or urine and all metabolites are measured in a single chromato...
The pyruvate uptake rate in inverted submitochondrial vesicles prepared from rat liver was optimized and further characterized; the potential inhibitory effects of the anticonvulsive drug valproic acid or 2-n-propyl-pentanoic acid (VPA), Δ4-valproic acid or 2-n-propyl-4-pentenoic acid and the r...
ObjectiveTo explore the influence of CYP2C9, CYP2A6, ACSM2A, CPT1A gene polymorphisms on valproic acid (VPA) and its role in metabolism-related liver dysfunction in order to guide the clinical safety and rational use of VPA.
Valproic acid and its unsaturated metabolite, 2-n-propyl-4-pentenoic acid, were found to inhibit strongly the metabolism of decanoic acid in homogenates of rat liver. Reductions in decanoate consumption in response to inhibitors were paralleled by decreases in the formation of octanoic and hexan...
Valproic acid (VA) is a branch chain fatty acid that is widely used to treat epilepsy and convulsion. Recent studies show that VA can also be used to treat migraine headaches, bipolar disorder, and other diseases such as Alzheimer disease. However, clinical treatment with VA may cause hepatotoxi...
Previous studies indicated that the enantiomers of thalidomide and its analogue EM 12 exhibit differing teratogenic potencies. Unfortunately, these substances proved to be unstable and racemised considerably, so that the intrinsic teratogenic potencies of the pure enantiomers were difficult to e...
Valproic acid (VPA) is a well-established anticonvulsant drug that has been increasingly used in the treatment of many forms of generalized epilepsy. Although there are many reports of adverse effects of VPA, studies focusing on the concentration–response relationships of VPA and its metabolite...
SummaryThe fluorescence spectra of the trivalent europium ion embedded in lanthanum orthovanadate in polycrystalline form reveal the existence of LaVO4 in its tetragonal form, i.e. having the zircon type structure. The lattice parameters of Eu3+ 10%: LaVO4 follow the linear variation vs the ioni...
To study the effect of substitution at the tetravalent ion, some barium lanthanide containing triple orthovanadates have been synthesised and structurally examined. The X-ray diffraction and the infrared spectroscopic data are analysed and interpretations are reported. It is observed that thoriu...
Neodymium Vanadate (NdVO4) nanostructures were successfully synthesized via a modified solid state method in the presence of ligand. These nanoparticles were further used as a photocatalyst. Primarily the best structural formations and smallest crystallite sizes of the systems were identified an...
We report a novel, simple synthetic route to uniform and highly crystalline rare earth orthovanadate (LnVO4, Ln = Ce, Pr, Nd, Sm, Eu, Gd, Tb, Dy, Er, or Y) nanocrystals prepared through the reaction between Ln(III)-acetate and a vanadyl sulfate aqueous solution in xylene in the presence of surfa...
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