The library of new N-substituted 4-(arylmethoxy)piperidines as dopamine transporter inhibitors was designed and synthesized. H-Bond donors in piperidine ring were found to be important for reduced locomotor activity in mice. 4-[Bis(4-fluorophenyl)methoxy]piperidine has IC50 17.0 ± 1.0 nm for do...

A series of hydroxamic acid derivatives bearing a cyclic amide/imide group as a linker and/or cap structure, prepared during our structural development studies based on thalidomide, showed class-selective potent histone deacetylase (HDAC)-inhibitory activity. Structure–activity relationship stu...

An efficient, general, and racemization free method of covalently attaching N α -Fmoc protected amino acids to solid supports for peptide synthesis is described. The process involves the preparation of 2,4-dichlorophenyl-N α -Fmoc-aminoacyl-4-oxymethyl-phenoxy acetates which can be used to dir...

This review surveys current knowledge of fatty acids (FAs) analysis, with an emphasis on the analysis of fatty acids in microorganisms in relation to microbial taxonomy, chemotaxonomy, and clinical practice. Aspects of fatty acid analysis in foods, drugs, and other products are also discussed, a...

A gas—liquid chromatographic method with electron-capture detection was developed for the determination of residues of 2,4-dichlorophenoxyacetic acid (2,4-D) and 4-chloro-2-methylpenoxyacetic acid (MCPA) in water as their 2,2,2-trichloroethyl esters, and the sensitivity was compared with that f...

A new highly efficient one-pot derivatization of medicinally important 9-aminoacridines (9-AA) at the amine position is described. Simple reductive amination and SNAr reaction using easily accessible starting materials give a fast entry to novel 9-AA derivatives for biological screening.

Trehalose-6-phosphate (T6P) is an important signaling metabolite involved in plant growth control that inhibits the sucrose nonfermenting-1-related protein kinase 1 (SnRK1), a key regulator of energy and carbon metabolism in plants. The quantification of T6P in plant tissues is fundamental to im...

An improved method was developed for the efficient, large-scale synthesis of α,α′-trehalose-6-phosphate starting with α,α′-trehalose. In the sequence, octa-trimethylsilylation of α,α′-trehalose is followed by selective removal of the 6-O-trimethylsilyl protecting group. Reaction of the ...

9H-carbazole is generated from incomplete combustion of diverse fossil fuels and biomass, in tobacco smoke and from industrial processes, while halogenated carbazoles have natural and anthropogenic sources.We analyzed 9H-carbazole and 14 halogenated carbazoles in dust samples from 14 schools, 13...

The chaperonin-containing t-complex polypeptide 1 (CCT, also known as TRiC) assists protein folding in an ATP-dependent manner. CCT/TRiC was mixed rapidly with different concentrations of ATP, and the amount of phosphate formed upon ATP hydrolysis was measured as a function of time using the cou...

Adding lubricant additives is a predictable method to decrease the frictional resistance in oil and gas drilling applications. In this work, tribological studies were carried out for drilling fluid with/without lubricant additives at different temperatures up to 200 °C and environmental pressur...

Background and PurposeKnowledge of commonly used medications (“Top 200”) is a common component of pharmacy curricula. This study assessed the impact of pre-pharmacy grade point average (GPA), timing of students' community introductory pharmacy practice experience (C-IPPE), C-IPPE practice...

Many applications in signal processing require the estimation of some parameters of interest given a set of observed data. More specifically, Bayesian inference needs the computation of a-posteriori estimators which are often expressed as complicated multi-dimensional integrals. Unfortunately, a...

Betaherpesvirus dUTPase homologs are core herpesvirus proteins, but little is known about their role during infection. Human cytomegalovirus (HCMV) UL72 and murine cytomegalovirus (MCMV) M72 have been designated dUTPase homologs, and previous studies indicate UL72 is dispensable for replication ...

SummaryMaintaining proteostasis in eukaryotic protein folding involves cooperation of distinct chaperone systems. To understand how the essential ring-shaped chaperonin TRiC/CCT cooperates with the chaperone prefoldin/GIMc (PFD), we integrate cryoelectron microscopy (cryo-EM), crosslinking-mass-...

SummaryThe hetero-oligomeric chaperonin of eukarya, TRiC, is required to fold the cytoskeletal protein actin. The simpler bacterial chaperonin system, GroEL/GroES, is unable to mediate actin folding. Here, we use spectroscopic and structural techniques to determine how TRiC promotes the conforma...

The total concentration of the norepinephrine metabolite 3-methoxy-4-hydroxyphenylethyl glycol (MOPEG) and propranolol concentration was measured in the medulla, pons, hypothalamus and thoracic spinal cord of conscious spontaneously hypertensive rats during the development of the antihypertensiv...

During early postnatal development rat pups were treated twice daily with the beta-adrenergic antagonist propranolol (15 mg/kg) in order to study the acute and long-lasting effects of early blockade of noradrenergic beta-mediated neurotransmission. Treatments from postnatal days 1–10 or days 11...

1.1. Rats were injected with d,l; 1- or d-propranolol, 50 mg/kg i.p.2.2. Levels of the monoamine metabolites 3-methoxy-4-hydroxyphenylglycol (MOPEG), homovanillic acid (HVA) and 5-hydroxy-indole-3-acetic acid (5-HIAA) were determined by mass fragmentography in regions of rat brain.3.3. After d,l...

(R,R′)-4′-Methoxy-1-naphthylfenoterol (MNF) promotes growth inhibition and apoptosis of human HepG2 hepatocarcinoma cells via cannabinoid receptor (CBR) activation. The synthetic CB1R inverse agonist, AM251, has been shown to block the anti-mitogenic effect of MNF in these cells; however, AM25...