N-methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine, a new cholinesterase and monoamine oxidase dual inhibitor

On the basis of N-((5-(3-(1-benzylpiperidin-4-yl)propoxy)-1-methyl-1H-indol-2-yl)methyl)-N-methylprop-2-yn-1-amine (II, ASS234) and QSAR predictions, in this work we have designed, synthesized, and evaluated a number of new indole derivatives from which we have identified N-methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine (2, MBA236) as a new cholinesterase and monoamine oxidase dual inhibitor.PostprintPostprintPeer reviewe

Modulation of internuclear communication in multinuclear Ruthenium(II) polypyridyl complexes

The syntheses and characterisation of a series of mononuclear and dinuclear ruthenium polypyridyl complexes based on the bridging ligands 1,3-bis-[5-(2-pyridyl)-1H-1,2,4-triazol-3-yl]benzene, 1,4-bis-[5-(2-pyridyl)-1H-1,2,4-triazol-3-yl]benzene, 2,5-bis-[5-(2-pyridyl)-1H-1,2,4-triazol-3-yl]thiophene, 2,5-bis-[5-pyrazinyl-1H-1,2,4-triazol-3-yl]thiophene are reported. Electrochemical studies indicate that in these systems, the ground state interaction is critically dependent on the nature of the bridging ligand and its protonation state, with strong and weak interactions being observed for thiophene- and phenylene-bridged complexes, respectively

Scaling-up Early Learning in Ethiopia: Exploring the Potential of O-Class

SDG Target 4.2 identifies ‘pre-primary education’ as a strategy to strengthen school readiness and contribute to the quality and outcomes of education, which is supported by the powerful evidence from evaluation research. The challenge faced by many countries is to deliver the proven potential of well-planned, quality programmes to scale. This working paper summarises Ethiopia’s growing commitment to pre-primary education and reports recent Young Lives engagement with the Ministry of Education in Ethiopia and other partners to support scale-up. Ethiopia’s most recent ambitious targets for early learning have been set out in the Fifth Education Sector Development Programme (ESDP V 2015), with pre-primary classes (known as O-Class) within primary schools being seen as the most rapid route to scale-up. The paper reports on the progress and the challenges in delivering ambitious targets. We report key findings from exploratory fieldwork on two key themes, namely the response of Regional Education Bureaus in planning, financing, management and ensuring human capacity for scale-up; and the potential of Ethiopia’s Colleges of Teacher Education to supply sufficient trained teachers to work with young children, especially in the rapidly expanding O- Classes. The final section draws on parallel experiences of other countries, notably Grade R in South Africa, and reports on six key challenges for scale-up; equity; age-appropriateness; cross- sectoral coordination; capacity building; and research and evidence. Other key challenges go beyond the scope of this working paper, notably the models for governance and financing that can deliver quality early education for all. While Ethiopia’s initiative to scale-up O-Class is a welcome indicator of policy commitment to SDG Target 4.2, we conclude that there is a risk that low quality pre-primary programmes will not deliver on the potential of early childhood education and that children (especially poor children) will be the losers

MICROWAVE-ASSISTED SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF SOME PYRAZOL-1-YLQUINOXALIN-2(1H)-ONE DERIVATIVES

3-Hydrazinoquinoxalin-2(1H)-one was prepared from quinoxaline-2,3-dione and subsequently used for the synthesis of some potentially biologically active 3-(pyrazol-1-yl)quinoxalin-2(1H)-one derivatives. While 3-(3,5-dimethylpyrazol-1-yl)quinoxalin-2(1H)-one showed a comparative effect with streptomycin, 3-(5-oxo-3-phenyl-4,5-di- hydropyrazol-1-yl)quinoxalin-2(1H)-one was found to be the most active with an MIC value of 7.8 μg/ml

2-Methylsulfanylbenzo[f]isoquinoline

S-Methylation of a 4-(naphth-2-yl)-β-thiolactam gives an intermediate 4-(naphth-2-yl) substituted 1-azetine which undergoes a [2+2] ring-opening followed by electrocyclic ring closure of the resulting 2-azadiene to give a benzo[f]isoquinolin

An iron(ii) spin-crossover metallacycle from a back-to-back bis-[dipyrazolylpyridine]

The syntheses of 4-mercapto-2,6-di(pyrazol-1-yl)pyridine (bppSH) and bis[2,6-di(pyrazol-1-yl)pyrid-4-yl]disulfide (bppSSbpp) are reported. In contrast to previously published “back-to-back” bis-[2,6-di(pyrazol-1-yl)pyridine] derivatives, which form coordination polymers with transition ions that are usually insoluble, bppSSbpp yields soluble oligomeric complexes with iron(II) and zinc(II). Mass spectrometry and DOSY data show that [{Fe(μ-bppSSbpp)}n]2n+ and [{Zn(μ-bppSSbpp)}n]2n+ form tetranuclear metallacycles in nitromethane solution (n = 4), although 1H NMR and conductivity measurements imply the iron compound may undergo more fragmentation than its zinc congener. Both [{Fe(bppSH)2]2+ and [{Fe(μ-bppSSbpp)}n]2n+ exhibit thermal spin-crossover in CD3NO2 solution, with midpoint temperatures near 245 K. The similarity of these equilibria implies there is little cooperativity between the iron centres in the metallacyclic structures

Synthesis and characterisation of ruthenium complexes containing a pendent catechol ring

A series of [Ru(bipy)₂L]⁺ and [Ru(phen)₂L]⁺ complexes where L is 2-[5-(3,4-dimethoxyphenyl)-4H-1,2,4-triazol-3-yl]pyridine (HL1) and 4-(5-pyridin-2-yl-4H-1,2,4-triazol-3-yl)benzene-1,2-diol (HL2) are reported. The compounds obtained have been characterised using X-ray crystallography, NMR, UV/Vis and emission spectroscopies. Partial deuteriation is used to determine the nature of the emitting state and to simplify the NMR spectra. The acid-base properties of the compounds are also investigated. The electronic structures of [Ru(bipy)₂L1]⁺ and Ru(bipy)₂HL1]²⁺ are examined using ZINDO. Electro and spectroelectrochemical studies on [Ru(bipy)₂(L2)]⁺ suggest that proton transfer between the catechol and triazole moieties on L2 takes place upon oxidation of the L2 ligand

Cymantrene–Triazole "Click" Products: Structural Characterization and Electrochemical Properties

We report the first known examples of triazole-derivatized cymantrene complexes (η5-[4-substituted triazol-1-yl]cyclopentadienyl)tricarbonylmanganese(I), obtained via a “click” chemical synthesis, bearing a phenyl, 3-aminophenyl, or 4-aminophenyl moiety at the 4-position of the triazole ring. Structural characterization data using multinuclear NMR, UV–vis, ATR-IR, and mass spectrometric methods are provided, as well as crystallographic data for (η5-[4-phenyltriazol-1-yl]cyclopentadienyl)tricarbonylmanganese(I) and (η5-[4-(3-aminophenyl)triazol-1-yl]cyclopentadienyl)tricarbonylmanganese(I). Cyclic voltammetric characterization of the redox behavior of each of the three cymantrene–triazole complexes is presented together with digital simulations, in situ infrared spectroelectrochemistry, and DFT calculations to extract the associated kinetic and thermodynamic parameters. The trypanocidal activity of each cymantrene–triazole complex is also examined, and these complexes are found to be more active than cymantrene alone

Travailler auprès de la personne âgée atteinte de démence: observations de huit jours à l'EMS "Les Tilleuls" : travail de Bachelor effectué dans le cadre de la formation à la Haute école de travail social de Genève

Ce travail de Bachelor a été distingué par le Prix Marie-Louise Cornaz 2014. À l’heure actuelle, la personne âgée atteinte de démence s’inscrit dans un contexte de peur. En effet, les pouvoirs publics s’alarment quant à l’augmentation incessante de cette maladie incurable ; les statistiques démontrent que les chiffres vont tripler dans les décennies à venir, s’élevant à 300’000 personnes atteintes en Suisse d’ici 2050. Force est de constater que cette thématique touche de près les EMS ; alors, comment travailler avec cette nouvelle population, indéniablement toujours plus présente en EMS ? Ainsi quatre axes ont été développés dans cette étude : - la maladie d’Alzheimer : qu’est-­ce que la démence ? - la communication : comment communiquer avec les personnes atteintes de démence ? ‐ la profession d’animateur socioculturel : quel est le sens de l’animation auprès de ce public ? ‐ les émotions : que fait l’animateur socioculturel de ses émotions ? Pour mener à bien cette recherche, j’ai utilisé la méthode inductive ; en partant du terrain, soit huit journées d’observations dans un EMS spécialisé dans l’accueil de personnes atteintes de démence, j’ai recueilli des données qui m’ont permis de formuler ma question de recherche et mes hypothèses. J’ai ensuite comparé mon analyse à différents auteurs traitant de ce thème. Ce travail permet, entre autres, de mettre en exergue l’importance de la profession d’animateur auprès de ce public si énigmatique, si complexe et par là difficilement accessible. En outre, cette étude atteste de l’importance d’un espace dédié à l’émotion du travailleur, afin de pouvoir être davantage centré sur l’autre dans sa pratique quotidienne

Developmental stage is an important factor that determines the antioxidant responses of young and old grapevine leaves under UV irradiation in a green-house.

The impact of UV irradiation was studied on photosynthesis, photosystem II photochemical yields and antioxidant responses using green-house grown grapevine (Vitis vinifera L. cv. Chardonnay) leaves. Supplemental UV irradiation (290-400 nm) was centred in the UV-B region, and corresponded to 8.95 kJ m-2 d-1 global (280-400 nm) or 8.04 kJ m-2 d-1 UV-B (280-315 nm) biologically effective dose. UV irradiation was applied daily and its effects were evaluated after 4-days. Younger (1-3 weeksold) leaves (YL) and older (4-6 weeks-old) leaves (OL) were affected differently, UV irradiation decreased their photochemical yields to 78% and 56%, respectively. Unlike OL, YL responded by an increase in UV-B absorbing pigment, anthocyanin and total phenolics contents. UV irradiation increased total antioxidant capacities in YL but not in OL. YL were also different in their ability to increase speciıic hydroxyl radical and singlet oxygen neutralizing capacities in response to the supplemental UV irradiation, which is reported here for the ıirst time. Our results suggest that the ability of maintaining photosynthesis under supplemental UV is not necessarily determined by base levels of antioxidants but rather by their inducibilities in response to the irradiation and emphasise the importance of comparing leaves of the same age in UV studies. Correlations between various antioxidant capacities, pigment contents and photosynthesis parameters were also examined. However, no single element of the defence system can be picked up as decisive factor of sensitivity to UV