Di-tert-butyl 2-benzoyl­hydrazine-1,1-dicarboxyl­ate

The crystal structure of the title compound, C17H24N2O5, was determined in the course of our studies on the preparation of two families of pseudopeptides, viz. hydrazino- and N-amino- peptides. The most significant inter­action in the crystal structure is a bifurcated inter­molecular N—H⋯O hydrogen bond

Boc-AzAla-Ala-OMe

The title compound (systematic name: tert-butyl 3-{[1-(methoxy­carbon­yl)eth­yl]amino­carbon­yl}-3-methyl­carbazate), C11H21N3O5, is a precursor for the study of a new class of foldamer based on aza/α-dipeptide oligomerization [Abbas et al. (2009 ▶). Tetra­hedron Lett. 50, 4158–4160]. The asymmetric unit consists of one mol­ecule in an extended conformation which is stabilized by inter­molecular N—H⋯O and C—H⋯O hydrogen bonding

Crystal Structure of Saccharomyces cerevisiae ECM4, a Xi-Class Glutathione Transferase that Reacts with Glutathionyl-(hydro)quinones

International audienceGlutathionyl-hydroquinone reductases (GHRs) belong to the recently characterized Xi-class of glutathione transferases (GSTXs) according to unique structural properties and are present in all but animal kingdoms. The GHR ScECM4 from the yeast Saccharomyces cerevisiae has been studied since 1997 when it was found to be potentially involved in cell-wall biosyn-thesis. Up to now and in spite of biological studies made on this enzyme, its physiological role remains challenging. The work here reports its crystallographic study. In addition to exhibiting the general GSTX structural features, ScECM4 shows extensions including a huge loop which contributes to the quaternary assembly. These structural extensions are probably specific to Saccharomycetaceae. Soaking of ScECM4 crystals with GS-menadione results in a structure where glutathione forms a mixed disulfide bond with the cysteine 46. Solution studies confirm that ScECM4 has reductase activity for GS-menadione in presence of glutathione. Moreover, the high resolution structures allowed us to propose new roles of conserved residues of the active site to assist the cysteine 46 during the catalytic act

Cyclic b-peptoids

The first synthesis of functionalized -peptoid macrocycles is reported. X-ray crystallographic structure of tetramer 9 reveals a C2-symmetrical derivative with unexpected all-cis-amide bonds and spatial disposition of the appendages toward the two opposite faces of the ring. Quantum calculations suggest that 9 is locked in this layout. These macrocycles constitute novel promising templates for multimeric ligation of biologically active ligands. The concept was exemplified by chemical decoration of tetramer 9 via "click" reaction

tert-Butyl 3-oxo-2-oxa-5-aza­bicyclo­[2.2.1]heptane-5-carboxyl­ate

The title compound, C10H15NO4, also known as N-tert-butyl­oxycarbonyl-allohydr­oxy-l-proline lactone, is quite similar to N-acetyl-allohydr­oxy-l-proline lactone [Lenstra, Petit & Geise (1979 ▶). Cryst. Struct. Commun. 8, 1023–1029], whereby both carbonyl groups point roughly in the same direction because of the trans conformation of the peptide bond

Carbohydrate-based peptidomimetics targeting neuropilin-1: synthesis, molecular docking study and in vitro biological activities

International audienceNeuropilin-1 (NRP-1), a transmembrane glycoprotein acting as a co-receptor of VEGF-A, is expressed by cancer and angiogenic endothelial cells and is involved in the angiogenesis process. Taking advantage of functionalities and stereodiversities of sugar derivatives, the design and the synthesis of carbohydrate based peptidomimetics are here described. One of these compounds (56) demonstrated inhibition of VEGF-A165 binding to NRP-1 (IC50 = 39 μM) and specificity for NRP-1 over VEGF-R2. Biological evaluations were performed on human umbilical vein endothelial cells (HUVECs) through activation of downstream proteins (AKT and ERK phosphorylation), viability/proliferation assays and in vitro measurements of anti-angiogenic abilities

Quelle R&D Mener pour le Développement Des Réseaux D'énergie De Demain ? Les Propositions de L'ancre en 2015

Feuille de route sur les réseaux électriques et stockage élaborée par le GP10 Réseaux et Stockages de l'Energie de l'ANCRECette feuille de route concerne les réseaux d’énergie électrique, de chaleur et de froid, les réseaux de gaz (hydrogène, gaz naturel), leurs stockages associés, ainsi que leurs couplages à venir dans le cadre de la transition énergétique et des évolutionsqui l’accompagneront, que ce soit sur les modes de production d’énergie ou sur l’évolution des usages.Le focus est porté sur les réseaux électriques qui seront les premiers impactés par cette transition énergétique. Hormisquelques éléments très spécifiques aux réseaux électriques (et qui seront notés dans le texte par une couleur différente)il est à souligner que la quasi-totalité des considérations et axes de R&D évoqués pour les réseauxélectriques et le développement de leur « intelligence » et/ou de leur flexibilité s’appliquentégalement aux autres réseaux d’énergie. Par ailleurs, si le groupe programmatique« Réseaux et Stockage » de l’ANCRE (GP10) s’est largement appuyé sur les nombreuses feuilles de route émises tant au niveau national, dont celles de l’ADEME, qu’européen, il a également souhaité s’en démarquer en insistantlargement et en détaillant les recherches scientifiques et technologiques à mener face aux verrous actuellement identifiés

An efficient route to acyclic C-nucleosides and fused-ring analogues of uridine from exo-glycals

International audiencebeta-Amino esters prepared from activated exo-glycals are transformed into acyclic C-nucleoside with a C-4-substituted uracil derivative that can be cyclized under Mitsututed conditions to provide it new Family of fused-ring analogues of uridine nucleoside in which the N-1 nitrogen atom is embedded in an amino sugar ring. An analogue of uridine of D-1 ibo configuration is prepared