Monitoring of aglycons of yew glycosides (3,5-dimethoxyphenol, myrtenol and 1-octen-3-ol) as first indicator of yew presence.

The toxicity of yew (Taxus spp) is well known from ancient times and is mainly due to taxins acting as inhibitors of calcium and sodium transport across the cell membrane of cardiac myocytes. The confirmation of yew taxins in body fluids can be carried out by liquid chromatography-tandem mass spectrometry (LC-MS/MS). However, before selecting this precise but expensive technique, an orientation test should be done to ascertain yew presence as toxic agent in the organism. As the 3,5-dimethoxyphenol (3,5-DMP), myrtenol and 1-octen-3-ol appear as glycosidically bound volatile compounds and are very yew specific, the detection of 3,5-DMP and the measurement of 1-octen-3-ol / myrtenol concentration ratio constitute reliable indicators of yew presence in forensic cases. The detection of these compounds is easily performed by gas chromatography-mass spectrometry (GC-MS) (SIM) after an enzymatic hydrolysis (β-glucosidase) allowing the release of volatile compounds from yew glycosides. Copyright �� 2012 John Wiley & Sons, Ltd.

Acreage Answers, June-July 2000, Vol. 1, no.3

Newsletter for those who reside on acreages in Iowa. Produced by the Iowa State University Extension Office.

Iowa Ag Review, June 1995, Vol. 1, no. 3

Iowa Ag Review is a quarterly newsletter published by the Center for Agricultural and Rural Development (CARD). This publication presents summarized results that emphasize the implications of ongoing agricultural policy analysis, analysis of the near-term agricultural situation, and discussion of agricultural policies currently under consideration.

Community College Leader Bulletin, Fall 2008, Vol. 1, Issue 3

Newsletter produced by the Iowa Department of Education, Community College unit. This report has information about staff, grants, statistical data, requirements and more.

Endeavors Update, Iowa Medicaid Enterprise, Vol. 1, Issue 3, November 30, 2010

The Iowa Medicaid Enterprise (IME) is an endeavor, started in 2005, to unite State staff with ���best of breed��� contractors into a performance-based model for administration of the Medicaid program.

A robust audio watermarking scheme based on MPEG 1 Layer 3 Compression

This paper describes an audio watermarking scheme based on lossy compression. The main idea is taken from an image watermarking approach where the JPEG compression algorithm is used to determine where and how the mark should be placed. Similarly, in the audio scheme suggested in this paper, an MPEG 1 Layer 3 algorithm is chosen for compression to determine the position of the mark bits and, thus, the psychoacoustic masking of the MPEG 1 Layer 3compression is implicitly used. This methodology provides with a high robustness degree against compression attacks. The suggested scheme is also shown to succeed against most of the StirMark benchmark attacks for audio.

1,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: synthesis, pharmacological evaluation and mechanistic studies

A series of 1,2,3,4-tetrahydrobenzo[h][1,6]naphthyridines differently substituted at positions 1, 5, and 9 have been designed from the pyrano[3,2-c]quinoline derivative 1, a weak inhibitor of acetylcholinesterase (AChE) with predicted ability to bind to the AChE peripheral anionic site (PAS), at the entrance of the catalytic gorge. Fourteen novel benzonaphthyridines have been synthesized through synthetic sequences involving as the key step a multicomponent Povarov reaction between an aldehyde, an aniline and an enamine or an enamide as the activated alkene. The novel compounds have been tested against Electrophorus electricus AChE (EeAChE), human recombinant AChE (hAChE), and human serum butyrylcholinesterase (hBChE), and their brain penetration has been assessed using the PAMPA-BBB assay. Also, the mechanism of AChE inhibition of the most potent compounds has been thoroughly studied by kinetic studies, a propidium displacement assay, and molecular modelling. We have found that a seemingly small structural change such as a double O ��� NH bioisosteric replacement from the hit 1 to 16a results in a dramatic increase of EeAChE and hAChE inhibitory activities (>217- and >154-fold, respectively), and in a notable increase in hBChE inhibitory activity (> 11-fold), as well. An optimized binding at the PAS besides additional interactions with AChE midgorge residues seem to account for the high hAChE inhibitory potency of 16a (IC50 = 65 nM), which emerges as an interesting anti-Alzheimer lead compound with potent dual AChE and BChE inhibitory activities.

1,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: synthesis, pharmacological evaluation and mechanistic studies

A series of 1,2,3,4-tetrahydrobenzo[h][1,6]naphthyridines differently substituted at positions 1, 5, and 9 have been designed from the pyrano[3,2-c]quinoline derivative 1, a weak inhibitor of acetylcholinesterase (AChE) with predicted ability to bind to the AChE peripheral anionic site (PAS), at the entrance of the catalytic gorge. Fourteen novel benzonaphthyridines have been synthesized through synthetic sequences involving as the key step a multicomponent Povarov reaction between an aldehyde, an aniline and an enamine or an enamide as the activated alkene. The novel compounds have been tested against Electrophorus electricus AChE (EeAChE), human recombinant AChE (hAChE), and human serum butyrylcholinesterase (hBChE), and their brain penetration has been assessed using the PAMPA-BBB assay. Also, the mechanism of AChE inhibition of the most potent compounds has been thoroughly studied by kinetic studies, a propidium displacement assay, and molecular modelling. We have found that a seemingly small structural change such as a double O ��� NH bioisosteric replacement from the hit 1 to 16a results in a dramatic increase of EeAChE and hAChE inhibitory activities (>217- and >154-fold, respectively), and in a notable increase in hBChE inhibitory activity (> 11-fold), as well. An optimized binding at the PAS besides additional interactions with AChE midgorge residues seem to account for the high hAChE inhibitory potency of 16a (IC50 = 65 nM), which emerges as an interesting anti-Alzheimer lead compound with potent dual AChE and BChE inhibitory activities.

Comment Samuel devint proph��te: Analyse du r��cit de 1 Samuel 3 dans son contexte

Le r��cit de 1 S 3 raconte comment une nuit Yhwh essaya �� plusieurs reprises de se r��v��ler au jeune Samuel, alors serviteur au sanctuaire de Silo. Instruit par son ma��tre ��li, le gar��on put finalement r��pondre �� Yhwh. Il devint alors r��cepteur d'un message divin. Yhwh annonce un ��v��nement effrayant qui va �� faire tinter les oreilles de quiconque en entendra parler ��. Au matin, Samuel rapporte la parole divine �� ��li, son ma��tre. �� la fin du r��cit le lecteur apprend que Yhwh continue de se ��v��ler �� Samuel. Voil�� en r��sum�� comment, selon le r��cit de 1 S 3, Samuel devint proph��te. Ce chapitre est interpr��t�� par les chercheurs de mani��res tr��s diff��rentes. On peut n��anmoins discerner deux tendances d'interpr��tation : a) 1 S 3 serait compos�� selon un certain genre litt��raire : il s'agirait d'un �� r��cit de vocation ��, voire d'un �� r��cit de r��ve d'incubation �� ou encore d'un �� r��cit de th��ophanie onirique ��. b) Le r��cit 1 S 3 a des liens forts avec le r��cit de 1 S 1-2, r��cit d'ouverture des livres de Samuel qui rapporte comment Samuel a ��t�� d��di�� au sanctuaire de Silo par sa m��re Anne et comment et dans quelles circonstances il a grandi au sanctuaire. ��tant donn�� ces liens, certains chercheurs estiment que les deux r��cits, �� un moment donn��, ont ��t�� r��unis en une seule narration portant sur la naissance de Samuel et sa jeunesse au sanctuaire de Silo. Cette narration de 1 S 1-3 aurait ��t�� �� l'origine ind��pendante des r��cits suivants (1 S 4-6) qui forment une entit�� autonome en commun avec 2 S 6, le soi-disant �� r��cit de l'arche ��. Le pr��sent article pr��sentera et discutera ces propositions en dialogue avec des id��es d'autres chercheurs ainsi que des suggestions personnelles. J'aborderai donc la question du genre du r��cit, et celle de la relation avec les r��cits qui l'encadrent. Pour cette seconde question il sera important d'examiner de tr��s pr��s l'oracle de Yhwh se trouvant au coeur du r��cit (v. 11-14) et de poser la question de l'��v��nement qu'il vise. �� la fin de la contribution les questions concernant le milieu et l'��ge du r��cit seront abord��es.

Synthesis of a tetrahydroimidazo-[2',1':2,3]thiazolo[5,4-c]pyridine derivative with Met inhibitory activity

A straightforward synthesis of the Met antagonist JLK1360 involving an alkylationcyclocondensation process using aminothiazole 1 and nitrophenacyl bromide 2, reduction of the nitro group, and coupling of the resulting tetracyclic aniline 5 with an appropriate N-acyl alanine derivative, is reported.

Synthesis of a tetrahydroimidazo-[2',1':2,3]thiazolo[5,4-c]pyridine derivative with Met inhibitory activity

A straightforward synthesis of the Met antagonist JLK1360 involving an alkylationcyclocondensation process using aminothiazole 1 and nitrophenacyl bromide 2, reduction of the nitro group, and coupling of the resulting tetracyclic aniline 5 with an appropriate N-acyl alanine derivative, is reported.

Espectro infravermelho e an��lise conformacional do composto 3-fenil-2-oxo-1,2,3-oxatiazolidina

The infrared (IR) spectra of the four distict conformers located on the multidimensional potential energy surface (PES) for the 3-phenyl-1,2,3-oxathiazolidine 2-oxide compound have been calculated using the semiempirical quantum-mechanical method PM3. The band spectra are reported and compared directly with the experimental spectrum. The IR intensities are shown to be much more sensitive to conformational changes than the vibrational frequencies and so, the theoretical analysis of the IR spectrum can be used as a tool for helping in the elucidation of the structure of heterocyclic compounds.