Hypoxic encephalopathy of the newborn is a major cause of long-term neurological sequelae. We have previously shown that CEP-701 (lestaurtinib), a drug with an established safety profile in children, attenuates short-term hyperexcitability and tropomyosin-related kinase B (TrkB) receptor activat...

ObjectivePatients with bladder cancer have responded poorly to oxaliplatin therapy in clinical trials. Blockade of receptor tyrosine kinases is considered a good strategy in cancer therapy. Our previous studies have demonstrated the crucial roles of brain-derived neurotrophic factor and its rece...

Lestaurtinib is an orally administered …

Ethametsulfuron methyl (methyl 2-[[[[(4-ethoxy-6-methylamino-1,3,5-triazine-2-yl)amino]carbonyl]amino]sulfonyl]benzoate, formerly DPX-A7881) is a sulfonylurea herbicide for postemergence broadleaf weed control in spring oilseed rape (Brassica napus L.), including canola varieties. Plant response...

Publisher SummaryThis chapter provides the basic synthesis paths routes for the manufacture of ethametsuIfuron–methyI, with a listing of the main raw materials and intermediates used in the synthesis of ethametsuIfuron–methyI. EthametsuIfuron–methyI is commercially known as Muster and it belo...

Under controlled environment conditions, ED50 values (dose required to reduce growth by 50%) determined from total plant dry weights in response to foliar-applied ethametsulfuron (DPX-A7881; (methyl-2-[(4-ethoxy-6-methylamino-1,3,5-triazin-2-yl)carbamoylsulfonyl]benzoate) were 148 and 0.85 g ai/...

The sorption and leaching of ethametsulfuron-methyl by an acidic soil, after organic amendment with humic acid (HA) and a commercial peat, were studied in batch and soil column experiments. Adsorption capacity (Kf) values, obtained by fitting the experimental data to the Freundlich equation, ran...

Leaching and degradation of the herbicide ethametsulfuron-methyl[methyl 2-[(4-ethoxy-6-methylamino-1,3,5-triazine-2-yl)carbamoylsulfamoyl]benzoate] in three soils were investigated under laboratory conditions. Ethametsulfuron-methyl was mobile on soils when tested using non-aged and aged soil co...

3-Substituted pentalongin derivatives possessing an acetal function at C-1 were synthesized by cyclization of acylmethylnaphthoquinones. The latter naphthoquinones were prepared starting from 2-dioxolanylnaphthoquinone by means of both a stoichiometric and a catalytic method deploying various py...

During the development of synthesis of acrylic pressure-sensitive adhesives, newly synthesized pyridinium derivatives were used by the UV-initiated polymerization quarantines of new polymer design for the synthesized self-adhesive acrylics with excellent performance, for which tack, peel adhesio...

The administration to mice of 1-methyl-4-(2′-methylphenyl)-1,2,3,6-tetrahydropyridine (2′-CH3-MPTP), a substituted analog of the dopaminergic neurotoxin MPTP caused even more dopaminergic toxicity than MPTP itself. Under conditions in which MPTP was relatively ineffective (i.e. two injections ...

The neurotoxic effects of 1-methyl-4-(2′-methylphenyl)-1,2,3,6-tetrahydropyridine (2′CH3-MPTP), a substituted analog of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, were studied in BALB/cJ mice. Moderate doses of 2′CH3-MPTP produced a greater depletion of dopamine (DA) in the striatum (45%) ...

The crystal structure for two salts of 3-methyl-4-(2,4,6-triphenylpyridinium-1-yl)-phenolate (1) with o-arsanilic (2-aminobenzene-arsonic) and perchloric acids were determined by X-ray diffraction. 1 was synthesized in order to break the symmetry of 4-(2,4,6-triphenylpyridinium-1-yl)-phenolate (...

Four adult marmosets were treated with increasing doses of 1-methyl-4-(2′-methylphenyl)-1,2,3,6-tetrahydropyridine (2′-methyl-MPTP) in the range 0.23–4.3 mg/kg i.p. to give a cumulative dose of 11.0–11.6 mg/kg over a 6–10 day period. After 4 days of treatment, and as the dosage was graduall...

1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and 1-methyl-4-phenylpyridinium cation (MPP+) are selective dopaminergic neurotoxins producing Parkinsonism. MPTP is activated by monoamine oxidase-B (MAO-B) to MPP+ that inhibits mitochondrial function. Molecules resembling MPTP which afford p...

The ionic liquids are remarkable molecules with exceptional properties and applications. The microwave assisted green method was used to synthesize (yield, up to 95%) a new series of pyridinium based ionic liquids (ILs); utilizing molecular hybridization of 2- and/or 3-methyl pyridine and severa...

Sixteen porphyrins, including neutral, anionic and cationic meso-(aryl)porphyrins and meso-(1-methyl-4-pyridinium)porphyrins were herein evaluated in terms of their photosensitizing properties against HaCaT keratinocytes. After an initial screening, the cationic porphyrins were studied in more d...

Nine novel {bis-4-[(3-alkyl-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-iminomethyl]-phenyl} [1,1′-biphenyl]-4,4′-disulfonates were synthesized and their structures were determined with spectral methods. Corrosion inhibitor activities of the title compounds were investigated using quantum mechanical meth...

A short and practical enantioselective synthesis of (+)-negamycin has been achieved in high enantio- and diastereomeric excess using an iterative Jacobsen’s hydrolytic kinetic resolution as the key step.

Sperabillin polymers, which have been shown recently to have antitumor activity, are new basic peptidyl polymers composed of a pseudo-peptide antibiotic, sperabillin A. The polymers, HP-2 (MW 9990), AP-2 (MW 20,100) and AB-2 (MW 35,000), were found to potently activate murine peritoneal macropha...