Ueber Aethyl- und Benzyl-Derivate des 1-Phenyl-3-Methyl-5-Pyrazolons.

Thesis (doctoral)--Universitat Jena.

Uber phosphorhaltige Derivate des 1-Phenyl-3-Methyl-5-Chlorpyrazols.

Thesis (doctoral)--Universitat zu Rostock.

Ueber die additionsfahigkeit des dimethyl-1-3-cyclohexenon-5.

Thesis (doctoral)--

Fragm. lat. I 60 - Psalterium (Ps 51,3 - 53,5)

Trägerband: Inc. oct. 67; Vorbesitzer: Kaspar (Casparus) Episcopius

Combinatorial solid phase synthesis of multiply substituted 1,4-benzodiazepines and affinity studies on the CCK2 receptor (Part 1)

One hundred sixty-eight multiply substituted 1,4-benzodiazepines have been prepared by a five-step solid-phase combinatorial approach using syn-phase crowns as a solid support and a hydroxymethyl-phenoxy-acetamido linkage (Wang linker). The substituents of the 1,4-benzodiazepine scaffold have been varied in the -3, -5, -7, and 8-positions and the combinatorial library was evaluated in a cholecystokinin (CCK) radioligand binding assay. 3-Alkylated 1,4-benzodiazepines with selectivity towards the CCK-B (CCK2) receptor have been optimized on the lipophilic side chain, the ketone moiety, and the stereochemistry at the 3-position. Various novel 3-alkylated compounds were synthesized and [S]3-propyl-5-phenyl-1,4-benzodiazepin-2-one, [S]NV-A, has shown a CCK-B selective binding at about 180 nM. Fifty-eight compounds of this combinatorial library were purified by preparative TLC and 25 compounds were isolated and fully characterized by TLC, IR, APCI-MS, and 1H/13C-NMR spectroscopy.

Hypervalent iodine in synthesis 92. A facile synthesis of 3-substituted-5,6-dihydroimidazo[2,1-b]thiazoles by cyclocondensation of alkynyl(phenyl)iodonium salts and imidazolidine-2-thione

A simple method for the synthesis of 3-substituted 5,6-dihydroimidazo[2,1-b]thiazoles is achieved by cyclocondensation of alkynyl(phenyl)iodonium salts with imidazolidine-2-thione.

A convenient synthesis of 5-benzylidenethiazolidine-2, 4-diones under microwave irradiation without solvent

A series of 5-benzylidenethiazolidine-2,4-diones was synthesised by the Knoevenagel condensation of aromatic aldehydes with thiazolidine-2,4-dione in the presence of catalytic amounts of piperidine and acetic acid under microwave irradiation without solvent in good yields.

The mammalian phosphatidylinositol 3-phosphate 5-kinase (PIKfyve) regulates endosome-to-TGN retrograde transport

The yeast gene fab1 and its mammalian orthologue Pip5k3 encode the phosphatidylinositol 3-phosphate [PtdIns(3)P] 5-kinases Fab1p and PIKfyve, respectively, enzymes that generates phosphatidylinositol 3,5-bisphosphate [PtdIns(3,5)P(2)]. A shared feature of fab1Delta yeast cells and mammalian cells overexpressing a kinase-dead PIKfyve mutant is the formation of a swollen vacuolar phenotype: a phenotype that is suggestive of a conserved function for these enzymes and their product, PtdIns(3,5)P(2), in the regulation of endomembrane homeostasis. In the current study, fixed and live cell imaging has established that, when overexpressed at low levels in HeLa cells, PIKfyve is predominantly associated with dynamic tubular and vesicular elements of the early endosomal compartment. Moreover, through the use of small interfering RNA, it has been shown that suppression of PIKfyve induces the formation of swollen endosomal structures that maintain their early and late endosomal identity. Although internalisation, recycling and degradative sorting of receptors for epidermal growth factor and transferrin was unperturbed in PIKfyve suppressed cells, a clear defect in endosome to trans-Golgi-network (TGN) retrograde traffic was observed. These data argue that PIKfyve is predominantly associated with the early endosome, from where it regulates retrograde membrane trafficking to the TGN. It follows that the swollen endosomal phenotype observed in PIKfyve-suppressed cells results primarily from a reduction in retrograde membrane fission rather than a defect in multivesicular body biogenesis.

La tradici?n oral como estrategia pedag?gica para el fortalecimiento de la etnoeducaci?n afrocolombiana inicial, en ni?os y ni?as de 3 a 5 a?os en el Centro de desarrollo infantil CDI El Guadual, municipio de Villa Rica, Cauca Fundaci?n "Casita de ni?os"

La tradici?n oral como estrategia pedag?gica para el fortalecimiento de la etnoeducaci?n afrocolombiana inicial, en ni?os y ni?as de 3 a 5 a?os en el Centro de desarrollo infantil CDI El Guadual municipio de Villa Rica, Cauca, es un proyecto de investigaci?n que busca aportar al fortalecimiento de las diversas identidades es culturales afrodescendientes, en ni?os y ni?as en educaci?n inicial, a trav?s de una pr?ctica pedag?gica que recupera y da valor a la oralidad, como parte de la herencia ancestral de la di?spora africana. Para el desarrollo del presente trabajo de grado, se parte de la pregunta: ? C?mo las pr?cticas ancestrales aportan al fortalecimiento de la Etnoeducaci?n Afrocolombiana inicial de ni?os y ni?as afrocolombianas de primera infancia en el CDI el Guadual, municipio de Villa Rica, Cauca? Cuyas respuestas se rastrean a partir de los aportes te?ricos de autores como el Dr. Carlos Velazco D?az, qui?n a trav?s de su trayectoria profesional ha rescatado diversas manifestaciones culturales de la regi?n, Heliana Portes de Roux, entre otros y las versiones que van de boca, en o?do narradas por las abuelas afrodescendientes, quienes son s?mbolo de autoridad y afecto.

A SUBSET OF 3´ TO 5´ EXORIBONUCLEASES ARE THE PRIMARY ENZYMES RESPONSIBLE FOR THE DEGRADATION OF PGPG IN CYCLIC DI-GMP SIGNALING

Bis-(3´-5´)-cyclic dimeric guanosine monophosphate, or cyclic di-GMP (c-di-GMP) is a ubiquitous bacterial second messenger that regulates processes such biofilm formation, motility, and virulence. C-di-GMP is synthesized by diguanylate cyclases (DGCs), while phosphodiesterases (PDE-As) end signaling by linearizing c-di-GMP to 5ʹ-phosphoguanylyl-(3ʹ,5ʹ)-guanosine (pGpG), which is then hydrolyzed to two GMPs by previously unidentified enzymes termed PDE-Bs. To identify the PDE-B responsible for pGpG turnover, a screen for pGpG binding proteins in a Vibrio cholerae open reading frame library was conducted to identify potential pGpG binding proteins. This screen led to identification of oligoribonuclease (Orn). Purified Orn binds to pGpG and can cleave pGpG to GMP in vitro. A deletion mutant of orn in Pseudomonas aeruginosa was highly defective in pGpG turnover and accumulated pGpG. Deletion of orn also resulted in accumulation c-di-GMP, likely through pGpG-mediated inhibition of the PDE-As, causing an increase in c-di-GMP-governed auto-aggregation and biofilm. Thus, we found that Orn serves as the primary PDE-B enzyme in P. aeruginosa that removes pGpG, which is necessary to complete the final step in the c-di-GMP degradation pathway. However, not all bacteria that utilize c-di-GMP signaling also have an ortholog of orn, suggesting that other PDE-Bs must be present. Therefore, we asked whether RNases that cleave small oligoribonucleotides in other species could also act as PDE-Bs. NrnA, NrnB, and NrnC can rapidly degrade pGpG to GMP. Furthermore, they can reduce the elevated aggregation and biofilm formation in P. aeruginosa ∆orn. Together, these results indicate that rather than having a single dedicated PDE-B, different bacteria utilize distinct RNases to cleave pGpG and complete c-di-GMP signaling. The ∆orn strain also has a growth defect, indicating changes in other regulatory processes that could be due to pGpG accumulation, c-di-GMP accumulation, or another effect due to loss of Orn. We sought to investigate the genetic pathways responsible for these growth defect phenotypes by use of a transposon suppressor screen, and also investigated transcriptional changes using RNA-Seq. This work identifies that c-di-GMP degradation intersects with RNA degradation at the point of the Orn and the functionally related RNases.

CIL 3.14147.5 – Trilingual dedication to the dei patriei and the Nile by C. Cornelius Gallus, first prefect of Egypt

Photographs and notes by A.E. Gordon

Creación de un Cd interactivo para el entrenamiento de la habilidad de memoria visual en niños entre 3 a 5 años

Tesis (Optómetra). -- Universidad de La Salle, Facultad de Ciencias de La Salud. Programa de Optometría, 2014