p-Butyroxybenzenediazonium fluoroborate 1 was shown to be a substrate of both acetylcholinesterase (AcChE) and butyrylcholinesterase (BuChE) with Michaelis constants of 6·10−5 M and 1.3·10−4 M, respectively. Upon incubation in the dark, 1 was able to discriminate between the two enzymes AcChE ...

Asymmetric syntheses of (−)-martinellic acid and (−)-4-epi-martinellic acid were achieved in 20 steps from commercially available starting materials using a diastereodivergent strategy. The conjugate addition of lithium (R)-N-allyl-N-(α-methyl-p-methoxybenzyl)amide to tert-butyl (E)-3-[2′-(N,N...

The asymmetric synthesis of 1-[2-hydroxy-3-(4-phenyl-1-piperazinyl)-propyl]-pyrrolidin-2-one 1 is described. Enantiomers of compound 1 were obtained using the Sharpless asymmetric dihydroxylation (AD) or hydrolytic kinetic resolution (HKR) methods. The enantiomers of compound 1, which were obtai...

cis-2,6-Bis-(methanolate)-piperidine oxovanadium(V) complexes are Lewis acids able to catalyze oxidative cyclization of alkenols by tert-butyl hydroperoxide (TBHP). Terminal dimethyl-substituted (prenyl-type) 4-pentenols bearing an alkyl or a phenyl group in position 1 afford under such conditio...

Self-consistent, full assignments of the 1H and 13C NMR spectra are reported for the macrocyclic antibiotics oligomycin-B and -C. Solution conformations, deduced from proton–proton and proton–carbon-13 coupling constants as well as from chemical shift considerations, are compared with X-ray da...

To evaluate the efficacy of Y-ART-3 as an antiviral drug for HIV infections, its anti-HIV activity was assessed in vitro in cell culture systems and in vivo in hu-PBL-SCID mice. The results indicated that Y-ART-3 invariably inhibited not only HIV-1, but also HIV-2 and SIV strains. Its mechanism ...

Two series of novel fluorinated aromatic polyamides were prepared from 2,2′-bis(4-amino-2-trifluoromethylphenoxy)biphenyl (2) and 2,2′-bis(4-amino-2-trifluoromethylphenoxy)-1,1′-binaphthyl (4) with various aromatic dicarboxylic acids using the phosphorylation polycondensation technique. The p...

2,2′,5,5′-Tetracarboxy- and 2,2′,5,5′-tetracarbamoyl-substituted biphenyls and also the 2,2′,3,3′,6,6′-hexacarboxy-substituted analogue behave as Siamese twins of terephthalic tectons in the single crystal self-assembly, giving rise to chiral 2D grid layers. A comparison has been made wit...

X-ray diffraction analysis revealed unexpected stereochemical features accompanying crystal self-assembly of the two title oligocarboxylic acids.

A catalytic double carboxylation of a bisboronate ester benzene was disclosed to synthesize terephthalic acid under a CO2 utilization approach. The double carboxylation was accomplished with several other bisboronate ester arenes to provide support for this being a general transformation. The do...

A description is given of the primary structure of a bovine adrenal medullary precursor protein (123 amino acids), containing a nonrepetitive galanin sequence, different in four amino acid positions from pig galanin, structural information deduced from the nucleotide sequence analysis of two cDN...

The neuropeptide galanin, which is widely expressed in brain and peripheral tissues, exerts a broad range of physiological effects. Pharmacological studies using peptide analogues have led to speculation about multiple galanin receptor subtypes. Since 1994, a total of three G-protein-coupled rec...

In a peptide concentrate, prepared from acid extracts of porcine brain, several galanin-like immunoreactive peptides were detected and two of these were purified. Characterization of the peptides by sequence analysis, mass spectrometry, and capillary zone electrophoresis identified them as a N-t...

RF-amide neuropeptides, with their typical Arg-Phe-NH2 signature at their carboxyl C-termini, belong to a lineage of peptides that spans almost the entire life tree. Throughout evolution, RF-amide peptides and their receptors preserved fundamental roles in reproduction and feeding, both in Verte...

Galanin message-associated peptide (GMAP) constitutes the C-terminal part of the precursor protein encoding also the biologically active neuropeptide galanin (GAL). We have raised antisera against a species-conserved portion of GMAP, and investigated the localization of GMAP-like immunoreactivit...

The galanin peptide family consists of the “parental” galanin, galanin-message-associated peptide (GMAP) which derives from the same peptide precursor gene product as galanin, galanin-like peptide (GALP) encoded by a different gene, and the recently discovered peptide alarin which is encoded b...

The galanin family currently consists of four peptides, namely galanin, galanin-message associated peptide, galanin-like peptide and alarin. Unlike galanin that signals through three different G protein-coupled receptors; GAL1, GAL2, and GAL3, binding at its N-terminal end, the cognate receptors...

In Aeromonas hydrophila, the gram-negative bacterial fish pathogen, PepO constitutes the thermoregulated outer membrane M13 family zinc endopeptidase, which is expressed maximally at 16 °C and is down-regulated above 30 °C. Cultivation of A. hydrophila at 16 °C enabled it to activate big endo...

BackgroundIn recent years, the literature associated with healthcare big data has grown rapidly, but few studies have used bibliometrics and a visualization approach to conduct deep mining and reveal a panorama of the healthcare big data field.

Alzheimer’s disease (AD) is thought to be caused by the accumulation of amyloid beta (Aβ) peptide within the brain. Endothelin-converting enzyme-2 (ECE-2), which is expressed in neural tissues, cleaves ‘big endothelin’ to produce the vasoconstrictor endothelin-1. ECE-2 also degrades Aβ. We ...