Substituted 3-hydroxyquinoline-2,4(1H,3H)-diones 3 were transformed into 3-acyloxy-1,3-dihydro-2H-indol-2-ones 4 and isomeric 4-acyl-1,4-dihydro-3,1-benzoxazin-2-ones 5. The influence of the substituents and the reaction conditions on the course of the reaction was studied. In the proposed mecha...

Benzoxazine derivatives are useful building blocks and display various biological activities. We serendipitously discovered and subsequently developed a new one pot method for the synthesis of 2-(dimethyl amino)/2-morpholino/2- (piperidin-1-yl)-4H-benzo[e][1,3]oxazin-4-ones from corresponding su...

We measured the genotoxic activities in two bacterial tests, the Salmonella/histidine assay (a reverse mutation assay) and the SOS chromotest (an assay for SOS induction in E. coli), of three 2-nitroanthrafurans: 2-nitroanthra[1,2-b]furan (R-7688), the isomeric compound 2-nitroanthra[2,1-b]furan...

- The corresponding cis- and trans-N-methyl- and N-benzyl-5,6- and 4,5-tetramethylenetetrahydro-l,3-oxazines (5a,b-8a,b)were synthesized from cis- and trans-N-methyl andN-benzyl-2- aminomethyl-1-cyclohexanols 1a,b,2a,b, from cis- and trans-N-methyl- and Nbenzyl -2-hydroxymethyl-1-cyclohexylamine...

New asymmetric syntheses of (−)-methyl shikimate 1 and (−)-5a-carba-β-d-gulopyranose 11 from d-arabinose through a common route which employed Mukaiyama-type intramolecular aldolization as a key step were described.

Neuropathic pain is a serious chronic disorder caused by lesion or dysfunction in the nervous systems. Endogenous nociceptin/orphanin FQ (N/OFQ) peptide and N/OFQ peptide (NOP) receptor [or opioid-receptor-like-1 (ORL1) receptor] are located in the central and peripheral nervous systems, the imm...

The asymmetric synthesis of methyl (E)-4-((1R,2S,3R)-3-amino-2-((E)-2-methoxycarbonyl-eten-1-yl)cyclohexyl)but-2-enoate 14 has been achieved from dimethyl (2E,7E)-nona-2,7-dienedioate 2. A key step is the asymmetric synthesis of 1-hydroxyoctahydro-1H-isochromene derivative 5 whose X-ray analysis...

Twenty purified dehydrogenases cloned from bakers’ yeast (Saccharomyces cerevisiae) and expressed as fusion proteins with glutathione (S)-transferase were tested for their ability to reduce three homologous cyclic β-keto esters. The majority of dehydrogenases reduced ethyl 2-oxo-cyclopentaneca...

The five suppressors SUP35, SUP43, SUP44, SUP45 and SUP46, each mapping at a different chromosomal locus in the yeast Saccharomyces cerevisiae, suppress a wide range of mutations, including representatives of all three types of nonsense mutations, UAA, UAG and UGA. We have demonstrated that ribo...

Omnipotent suppression is a well-established phenomenon in yeast and bacteria in which nonsense mutations are misread. Wild-type (wt) suppressors are presumed to be involved in ensuring the fidelity of translation. We report a human homolog to wt yeast omnipotent suppressor 45 which shares 63% i...

3H-Cyclonona[def] biphenylene, 6, was deprotonated with n-butyllithium to form the mono-trans anion 7. This anion was fully delocalized and aromatic, with the interior proton having a 1H NMR absorption at -2.79 ppm. This downfield shift was attributed to the proton being in the middle of a ring ...

BackgroundThe association of plasma factor XIII (FXIII) level with venous thromboembolism (VTE) is still controversial and the effect of sex and FXIII B subunit (FXIII-B) polymorphisms in this respect have not been explored.

3-(S-Cysteinyl)glutaric acid, S-(1-methyl-2-carboxyethyl)cysteine, and S-(1,2-dimethyl-2-carboxyethyl)cysteine have been found in normal human urine as minor components.

Fourphit (4-isothiocyanato-1-[1-phenylcyclohexyl]piperidine), an acylating phencyclidine derivative that irreversibly inhibits stimulant binding to the dopamine transporter in vitro (Schweri et al., J. Pharmacol. Exp. Ther. 261:936–942, 1992), was tested in rats for its ability to block the inc...

A new hair-dye coupler, 2-(2′,4′-diaminophenoxy)ethanol was analyzed for its potential mutagenic activity in different genotoxic assays, namely gene reverse mutations in Salmonella typhimurium, forward mutations in the yeast Schizosaccharomyces pombe, and in the V79 Chinese hamster cell line g...

We investigated the effects of pramipexole, a potent dopamine receptor D2/D3 agonist, on light-induced retinal damage in mice, H2O2-induced retinal pigment epithelium ARPE-19 cell injury in humans, and hydroxyl radical scavenging activity in a cell-free system. Pramipexole (0.1 and 1 mg/kg body ...

Parkinson’s disease (PD) is associated with symptoms such as tremor and bradykinesia which, together with a rigorous dosing regimen, can place an untenable burden on patients. These issues underscore the need for triggerable, modulated drug delivery systems. Currently, pramipexole (PRX) is the ...

In the present study the effect of pramipexole alginate nanodispersion (PAND) was studied on the transgenic Drosophila exhibiting the PD symptoms. The PD flies were allowed to feed on the diet having PAND at final concentration of 1, 2 and 3 μM. A dose dependent significant delay in the loss of...

The dopamine agonist pramipexole is cleared predominantly by the kidney with a major contribution of active renal secretion. Previously the organic cation transporter 2 (OCT2) was shown to be involved in the uptake of pramipexole by renal tubular cells, while the mechanism underlying efflux into...

Study objectivesThe objective of this study is to assess adherence and persistence of ropinirole, pramipexole, and gabapentin; to investigate factors associated with non-adherence and non-persistence in restless legs syndrome (RLS) patients.