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1.
Anal Sci ; 22(9): 1265-8, 2006 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-16966823

RESUMEN

The Japan Society for Analytical Chemistry has developed some new plastic certified reference materials (CRMs) for the analysis of mercury in polyester disks using XRF analysis. These CRMs (named as JSAC 0621-0625) were prepared by casting polyesters including a toluene solution of organometallic compounds as a standard. Concentrations of the five levels of mercury ranged from 0 to 250 mg/kg. Homogeneity tests of prepared disks had shown excellent results. Interlaboratory comparison study for the certification was performed by 15 laboratory participants. The z-scores in robust statistical method was applied for the evaluation of outliers. The certified values were assigned after discarding outliers. The uncertainties of certified values were determined as the confidence levels of 95%.

2.
Bioorg Med Chem Lett ; 16(12): 3323-9, 2006 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-16630723

RESUMEN

Design, synthesis, and in vitro and in vivo evaluation of a series of antipsoriatic antedrugs having 16-en-22-oxa-vitamin D3 are described. Among the seven compounds examined, two are promising: ester 5c and amide 5f, both of which exhibit greater potent antiproliferation activity with lessened calcemic activity than the presently prescribed maxacalcitol (2).


Asunto(s)
Colecalciferol/química , Colecalciferol/uso terapéutico , Diseño de Fármacos , Psoriasis/tratamiento farmacológico , Animales , Colecalciferol/síntesis química , Colecalciferol/farmacología , Estructura Molecular , Ratas , Relación Estructura-Actividad
3.
Anal Sci ; 22(2): 225-8, 2006 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-16512412

RESUMEN

A rapid sample-digestion method for the determination of toxic metals, cadmium, chromium, and lead, in polyethylene and polyvinyl chloride has been developed by using a microwave oven for household use. An appropriate amount of the sample taken in a PTFE decomposition vessel was mixed with nitric acid or nitric and sulfuric acids. The vessel was heated in a microwave oven by a predetermined operating program. The digested sample was diluted to a definite volume with water after evaporating most of the nitric acid. The precipitate, if formed, was filtered off by a membrane filter. The metals were determined by ICP-AES. The sample digestion required 5 min (for 20-mg sample) to 25 min (for 60-mg sample). The analytical results obtained for cadmium, chromium, and lead in a polyethylene certified reference material, BCR-680, digested with nitric acid, were in good agreement with the certified values.


Asunto(s)
Técnicas de Química Analítica/instrumentación , Técnicas de Química Analítica/métodos , Microondas , Plásticos/química , Cadmio/química , Cromo/química , Ácido Nítrico/química , Polietileno/química , Polietilenos/química , Ácidos Sulfúricos/química , Oligoelementos , Agua/química , Rayos X
4.
Bioorg Med Chem ; 14(6): 1838-50, 2006 Mar 15.
Artículo en Inglés | MEDLINE | ID: mdl-16307885

RESUMEN

A series of 16-en-22-oxa-derivatives of vitamin D3 based on the structure of maxacalcitol (2) were prepared. Maxacalcitol is currently used topically for the treatment of psoriasis and is recognized as the most successful antedrug of natural vitamin D(3) because it retains the original antiproliferative activity of calcitriol without increased calcemic activity. We introduced 16-olefinic functionality to accelerate the oxidative metabolism of the drug in liver, presumed to be essential for the reduction of calcemic activity, and modified the side-chain moiety by placing the 22-oxygen on the more labile allylic carbon center. Novel 22-oxa analogs (7a-i), carrying either the 24-alkynyl bond or 24-hydroxy functionality in addition to the 16-double bond were synthesized and their pharmacokinetics were evaluated.


Asunto(s)
Psoriasis , Vitamina D/análogos & derivados , Vitamina D/química , Animales , Proliferación Celular/efectos de los fármacos , Células Cultivadas , Evaluación Preclínica de Medicamentos , Células Epidérmicas , Epidermis/efectos de los fármacos , Humanos , Queratinocitos/efectos de los fármacos , Masculino , Microsomas Hepáticos/efectos de los fármacos , Modelos Moleculares , Estructura Molecular , Psoriasis/tratamiento farmacológico , Ratas , Relación Estructura-Actividad , Vitamina D/farmacocinética
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