Analyses of trace amounts of alkene vapours present in exhaled breath are becoming important in clinical research related to inflammatory bowel disease, IBD, currently affecting over 1 million patients in the USA and 2.5 million in Europe. Concentrations of alkenes have been previously found to ...

Most of the structural assignments presented in this paper were based on the conformation of angustifoline selectively deuterated at the 13β position (13β2H I). To confirm the absolute stereoselectivity of the reaction introducing 2H at 13C on the β face, 13β2H I was transformed into four de...

Voltammetric behavior of omeprazole on chemically unmodified boron-doped diamond electrode was investigated. Omeprazole is possible to oxidize and reduce in various supporting electrolytes. Both processes are strongly dependent on pH value of the solution. Well defined oxidation and reduction si...

Although several studies have assessed the short-term effect of dietary supplements on the treatment and prevention of gastric ulceration in horses, few have assessed the response over a duration of more than 30 days. A blinded randomized noninferiority clinical trial was conducted using 42 Thor...

Natural or synthetic small molecules (

PurposeThe purpose of this study was to assess whether prophylaxis for digestive disorders with omeprazole is a risk factor for adverse drug events (ADEs) and kidney impairment.

Modified-release oral dosage forms are commonly used in pharmaceutics to delay or sustain the release of drugs. Nowadays, they are only marketed as solid dosage forms such as capsules or tablets. Therefore, the development of a liquid oral dosage form with modified-release properties has been ke...

α-Melanotropin (α-MSH, i.e. α-melanocyte stimulating hormone), tridecapeptide (Ac-Ser1-Tyr-Ser-Met-G1u5-His-Phe-Arg-Trp-Gly10-Lys-Pro-Val13-NH2), has been extensively studied to understand structure–activity relationships. The core sequence (His-Phe-Arg-Trp) is conserved in several species a...

[Met5]enkephalin-Arg-Phe (Tyr-Gly-Gly-Phe-Met-Arg-Phe) was modified with the methyl esther of melphalan (Mel; 4-bis(2-chloroethyl)amino-l-phenylalanine) and the resulting compounds were studied for their opioid binding properties in guinea pig and rat brain membranes. Three new peptides, with a ...

Hip-Arg-Phe-, Hip-Phe-Arg-and Hip-His-Leu-cleaving dipeptidyl carboxypeptidase activities were measured in the supernatant (S2) and pellet (P2) fractions obtained by ultracentrifugation of human adrenal tumor preparations. Negligible enzyme activity was found in cortical tumor whereas highly sig...

Melanoma skin cancer is the fastest growing cancer in the US [1]. A great need exists for improved formulations and mechanisms to prevent and protect human skin from cancers and other skin damage caused by sunlight exposure. Current efforts to prevent UV damage to human skin, which in many cases...

Diisopropylthiourea (DPT), an intermediate of a widely used cephalosporin, has been found to be one of the most refractory components in cephalosporin synthesis wastewater. This compound cannot be completely removed by conventional biological processes due to its antimicrobial property. Ionizing...

A series of mixed N-heterocycles/N-heterocyclic carbene palladium(II) allyl complexes with general formula [(NHC)Pd(η3-allyl)]2(μ2-N-heterocycles)(BF4)2 were prepared in one pot based on anion metathesis of (NHC)Pd(η3-allyl)Cl complexes and then ligand replacement with N-heterocycles [N-heter...

BackgroundPenumbra salvage from infarction by early reperfusion within the time window is the target of acute ischemic stroke therapies. Although the penumbral imaging is potently usable in clinic trial, additional work needs to be performed to advancing the field with better-defined, evaluated,...

The utility of the diaminoquinazoline derivative CP-100,356 as an in vivo probe to selectively assess MDR1/BCRP-mediated drug efflux was examined in the rat. CP-100,356 was devoid of inhibition (IC50 >50 µM) against major human P450 enzymes including P4503A4. In human MDR1-transfected MDCKII ce...

Effects of the new cardiotonic and selective β1-adrenergic agonist TA-064, (−)-(R)-1-(p-hydroxyphenyl)-2-[(3,4-dimethoxyphenethyl)amino]ethanol, on circulating concnetrations of glucose, lactate, free fatty acids (FFA), glycerol, cyclic AMP and the pancreatic hormones insulin (IRI) and glucagon...

In addition to the known dihydroxystyrylguanidine alkaloid tubastrine (1), five new dimers, orthidines A–E (2–6) and the biosynthetically unrelated 1,14-sperminedihomovanillamide (orthidine F, 7) were isolated from the New Zealand ascidian Aplidium orthium. The structures of the new compounds,...

A general five-step synthesis of a short library of benzo[7,8]indolizinoquinolinine analogues of the topoisomerase-1 (topo-1) poison rosettacin and 22-hydroxyacuminatine alkaloids from DMAD and ortho-ketoanilines is reported. This consists on successively, the tandem aza-Michael addition/cyclode...

A new series of 3-(1-(3,4-dimethoxyphenethyl)-4,5-diphenyl-1H-imidazol-2-yl)-1H-indole derivatives (5a-5j) are conveniently synthesized and characterized by IR, 1H NMR and 13C NMR spectral techniques. The compound 5f was also confirmed by single crystal XRD analysis and optimized bond parameters...

Evidence for the structure of the antitumor alkaloid leurosine is presented, together with the explanations for the mass spectral fragmentation patterns observed. Nuclear magnetic resonance spectroscopic data support the proposal that leurosine contains an epoxide moiety, and is closely related ...