Xanthomegnin, a mutagenic mycotoxin best known as an agent of nephropathy and death in farm animals exposed to food-borne Penicillium and Aspergillus fungi, was first isolated about 35 y ago as a diffusing pigment from cultures of the dermatophyte, Trichophyton megninii. This study investigates ...
Here, we aimed to discriminate the Trichophyton rubrum and Trichophyton mentagrophytes complexes, via detection of xanthomegnin using HPLC. We concluded that it is not a reliable technique for discriminating the two complexes, because strains belonging to both T. rubrum and T. mentagrophytes com...
Grignard reaction of ethyl 3-(3,5-dimethoxyphenyl)-propionate (4) followed by cyclodehydration of the carbinol (5) with conc H2SO4 gave 4,6-dimethoxy-3,3-dimethylindane (6). Oxidation of the indane (6) with CrO3-pyridine complex in methylene chloride gave 4,6-dimethoxy-3,3-dimethylindan-1- one (...
Publisher SummaryDepsides, depsidones, and depsones that occur in lichens are described in this chapter. Depsides and depsidones are present in lichens in varying concentrations up to 5% dry weight. Spectroscopic methods applied to the structural elucidation of depsides are reviewed. Mass spectr...
A combined experimental and theoretical analysis of on molecular structure, vibrational spectra and HOMO-LUMO analysis of 1-{3-(4-chlorophenyl)-5-[4-(propan-2-yl)phenyl]-4,5-dihydro-1H-pyrazol-1-yl}-ethanone is reported. The equilibrium geometry and vibrational wavenumbers have been computed usi...
Highly fluorescent trans- and cis-tris(fluorenylphenylamino)benzene stereo-isomeric derivatives, trans- and cis-tris(DPAF-C9), respectively, were designed and synthesized to minimize facile planar fluorene ring stacking in the solid state during thin-film device fabrications. Resulting tris-cup ...
1,2-Bis(pentaphenylphenyl)benzene (2) was synthesized by the cycloaddition of 1,2-bis(phenylethynyl)benzene and tetracyclone. Its X-ray structure was determined, and the molecule adopts a C2-symmetric conformation in the crystal. Monomethoxy and dimethoxy derivatives of compound 2 were also prep...
Peroral administration of tacrine, the first acetylcholinestearse inhibitor licensed for the treatment of Alzheimer’s disease, is associated with low bioavailability, due to an extended first-pass methabolism, short elimination half-life and hepatotoxicity. Nasal drug delivery may reduce the de...
ObjectivesWe examined the effects of two dopamine agonists, cabergoline and rotigotine, on tacrine-induced tremor and c-Fos expression in rats.
A series of new indole-3-acetic acid (IAA)-tacrine hybrids as dual acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) inhibitors were designed and prepared based on the molecular docking mode of AChE with an IAA derivative (1a), a moderate AChE inhibitor identified by screening our compoun...
A series of novel tacrine-phenolic acid dihybrids and tacrine-phenolic acid-ligustrazine trihybrids were synthesized, characterized and screened as novel potential anti-Alzheimer drug candidates. These compounds showed potent inhibition activity towards cholinesterases (ChEs), among of them, 9i ...
A new series of tacrine-coumarin hybrids linked to 1,2,3-triazole were designed, synthesized, and tested as potent dual binding site cholinesterase inhibitors (ChEIs) for the treatment of Alzheimer’s disease (AD). Among them, compound 8e was the most potent anti-AChE derivative (IC50 = 27 nM) a...
In the early 1950s, tacrine was used experimentally to reverse cholinergic coma in animals. In 1993, the US Food and Drug Administration approved tacrine for the treatment of mild to moderate Alzheimer's disease. Tacrine causes reversible acetylcholinesterase inhibition in the brain, and th...
The present study deals with the physicochemical characterization of solid forms of tacrine monohydrochloride (TCR), a centrally active reversible acetylcholinesterase inhibitor for treating the symptoms of mild to moderate Alzheimer's disease, obtained by recrystallization of hot saturated...
The aim of present investigation is to evaluate the feasibility of transdermal iontophoretic delivery of tacrine hydrochloride in Sprague Dawley (SD) rats using anodal iontophoretic patches and to correlate plasma tacrine concentration profiles to in vitro tacrine permeation flux. In vitro skin ...
Sweeteners improve the dietary properties of many foods. A candidate for a new natural sweetener is 5-ketofructose. In this study a fed-batch process for the production of 5-ketofructose was developed. A Gluconobacter oxydans strain overexpressing a fructose dehydrogenase from G. japonicus was u...
When quinoxaline-N-oxide 1 is reacted with KCN and benzoyl chloride in water (the Reissert reaction) or methanol, the products are 2-,5- and 6- chloroquinoxaline (the latter being the major product: 42±6 %) and small amounts of 2-cyanoquinoxaline. Using three equivalents of trimethylsilyl cyani...
A mild and efficient synthetic protocol for the oxidation of benzil-α-arylimino oximes 3 utilizing iodobenzene diacetate (IBD) as an oxidizing agent has been developed. Oximes 3, obtained by the condensation of (E)-benzil monoxime 2 with various appropriately substituted anilines 1, on treatmen...
The PVC membrane containing 2,3-diphenylquinoxaline-4′,4″-dioxytriethylene glycol (PQTEG) as a suitable ionophore, presents a linear dynamic range of 1.0 × 10− 6–1.0 × 10− 2 M with a Nernstian slope of 29.9 mV per decade and a detection limit of 6.7 × 10− 7 M. The response time is quick (s...
The new iridium complexes containing a derivative of 2,3-diphenylquinoxaline as an emitting ligand were synthesized, and their photophysical properties were investigated. The complexes prepared in this study were bis(6-F-2,3-di(p-fluorophenyl) quinoxalinato)iridium acetylacetonate (Ir(6-F-2,3-dp...
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