Mangancarbonyl Mn 2 (CO) 10 zeigt in seinem chemischen Verhalten Beziehungen zum homologen Rheniumcarbonyl, so der Existenz charakteristischer Halogenopentacarbonyle Mn(CO) 5 Halg, wie auch Kobaltcarbonyl, namentlich hinsichtlich seiner Reaktion mit Alkalilaugen, die Pentacarbonylmanganat [Mn(CO) ] – führt. Von letzterem leiten sich Salze komplexen Kationen ab; Alkalisalze ]Na entstehen unmittelbar aus dem Pentacarbonyl und Alkalimetall. Im übrigen ein bemerkenswertes Sonderverhalten...

A m y l e das VOII uns dargestellte Amylen ideiitisctr und mit welchen es nur isomer ist; gleichzeitig wollen wir den existirenden AnscbRuungen iiber die

Phytopharmaceuticals prepared from flowerheads of Arnica montana Spanish origin and the new type "Arbo", which can be easily economically cultivated, were studied for their capability to impair activation transcription factors NF-kappa B NF-AT. Both proteins are responsible genes encoding various inflammatory mediators. Additionally, influence on release cytokines IL-1 TNF-alpha examined. The inhibitory activities correlate with quantitative qualitative content sesquiterpene lactones (Sls)....

A series of polysubstituted pyridin-4-yl imidazole inhibitors p38 MAP (mitogen-activated protein) kinase was prepared as small molecular anticytokine agents and drug candidates for the treatment chronic inflammatory diseases. The contribution substituents at pyridinyl moiety to selective inhibition without concomitant cytochrome P450 interaction evaluated. Placement a 1-phenylethyl (7e, p38: IC50 0.38 μM) or acetyl substituent exocyclic nitrogen several 2-aminopyridine imidazoles led...

Regioselective synthetic approaches to tetrasubstituted imidazoles (see picture) are reported. These highly substituted heterocycles potent inhibitors of cytokine release and therefore interesting candidates for anti-inflammatory drugs. Supporting information this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2002/2002/z18173_s.pdf or from author. Please note: The publisher not responsible content functionality any supporting supplied by authors. Any queries...

A series of novel 5-substituted UDP-glucose derivatives with interesting fluorescent properties and potential applications as sensors for carbohydrate-active enzymes is reported. An efficient synthesis the target molecules was developed, centred around Suzuki–Miyaura reaction (hetero)arylboronic acids 5-iodo UDP-glucose. Interestingly, optimised cross-coupling conditions could also be applied successfully to 5-bromo UMP, but not

Novel 2,4,5-trisubstituted imidazole derivatives were prepared as potential anticytokine agents. Thirty-seven compounds tested on their ability to inhibit the release of tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) from peripheral blood mononuclear cells (PBMC) or human whole blood. SARs (structure activity relationships) for substituents at 4 5 position core similar those described other inhibitors cytokine p38 MAP (mitogen-activated protein) kinase. Starting benzylsulfanyl 2b...

The direct structural modification of GDP-mannose via the bromination and Suzuki-Miyaura cross-coupling unprotected sugar-nucleotide, to produce 8-substituted fluorescent analogues GDP-mannose.

A convenient and high yielding procedure for the Suzuki–Miyaura cross-coupling of unprotected bromo- chlorotryptophans in water provides fluorescent aryltryptophans.

Galactosyltransferases (GalT) are important molecular targets in a range of therapeutic areas, including infection, inflammation, and cancer. GalT inhibitors therefore sought after as potential lead compounds for drug discovery. We have recently discovered new class with novel mode action. In this publication, we describe series analogues which provide insights, the first time, into SAR inhibition. also report that C-glycoside, designed chemically stable analogue most potent inhibitor...

A novel, fluorescent NAD derivative is processed as substrate by three different NAD-consuming enzymes. The new probe has been used to monitor enzymatic activity in a continuous format changes fluorescence and, one case, directly visualize alternative reaction pathways.

New inhibitor chemotypes for glycosyltransferases, which are not structurally derived from either donor or acceptor substrate, being reviewed.

We report a simple and high-yielding two-step procedure for the preparation of 8-arylated guanosine mono- triphosphates (8-aryl GXPs). The key step our synthesis is Suzuki–Miyaura coupling unprotected 8-bromo GMP GTP with various arylboronic acids in aqueous solution. 8-bromoguanosine 5′-phosphates required as cross-coupling substrates were prepared from via an optimised Yoshikawa procedure.

A concise synthesis of five new analogues the second messenger cADPR (cyclic adenosine 5'-diphosphate ribose) is presented. The synthetic plan centered around key derivative 8-Br-N1-cIDPR 8-Br-inosine ribose, 2), which was prepared in only three steps from IMP (inosine 5'-monophosphate) via an unusual enzymatic cyclization reaction. enhanced stability 2 allowed for direct modification this cyclic dinucleotide at 8 position, providing unsubstituted parent N1-cIDPR (4) as well 8-phenyl (5),...

The structural features needed for antagonism at the cyclic ADP-ribose (cADPR) receptor are unclear. Chemoenzymatic syntheses of novel 8-substituted 2′-deoxy-cADPR analogues, including 8-bromo-2′-deoxy-cADPR 7, 8-amino-2′-deoxy-cADPR 8, 8-O-methyl-2′-deoxy-cADPR 9, 8-phenyl-2′-deoxy-cADPR 10 and its ribose counterpart 8-phenyl-cADPR 5 reported, improved established antagonists 8-amino-cADPR 2 8-bromo-cADPR 3. Aplysia californica ADP-ribosyl cyclase tolerates even bulky 8-phenyl-nicotinamide...