Structure-Activity Relationship Explorations and Discovery of a Potent Antagonist for the Free Fatty Acid Receptor 2

Free fatty acid receptor 2 (FFA2) is a sensor for short-chain fatty acids that has been identified as an interesting potential drug target for treatment of metabolic and inflammatory diseases. Although several ligand series are known for the receptor, there is still a need for improved compounds. One of the most potent and frequently used antagonists is the amide-substituted phenylbutanoic acid known as CATPB ( 1 ). We here report the structure-activity relationship exploration of this compound, leading to the identification of homologues with increased potency. The preferred compound 37 (TUG-1958) was found, besides improved potency, to have high solubility and favorable pharmacokinetic properties.     

First RAFT polymerization of captodative 2-acetamidoacrylic acid (AAA) monomer: An experimental and theoretical study

A capto-dative monomer, 2-acetamidoacrylic acid (AAA), was homopolymerized through RAFT polymerization method using 2-(2-cyanopropanyl dithiobenzoate) (CPDB) as a chain transfer agent and AIBN free radical initiator in DMF at 70 °C. DFT calculations were performed in the selection of the CTA for this unique monomer as well as to elucidate the influence of cd-stabilized growing radical on the kinetic parameters in comparison to methacrylic acid (MAA) and N-(prop-1-en-2-yl)acetamide (NPAA), which represent the captive and dative groups of AAA, respectively. K_eq for these three monomers is in the order of AAA < MAA < NPAA. While k_β > k_−add for NPAA and MAA, for AAA k_−add is about four orders of magnitude larger than k_β. This is the major disadvantage in the RAFT process of AAA using CPDB. Yet, poly(AAA) could be achieved with PDI as low as 1.49. Molecular weight of the polymer can be tuned by the monomer/AIBN ratio. First block copolymers of AAA with MAA and MMA using poly(AAA) as a macro-CTA were also synthesized, indicating the presence of active chain ends.     

New Pilot Plant Studies at the Budapest Waterworks

The quality of water provided by the Budapest Waterworks should comply with the standards prescribed by the European Community. According to these provisions, on one of the major water-producing regions (Csepel Island), rows of wells of 60,000 m³/day yield have been closed recently, and in the immediate future further plants would have been closed because of the high iron and manganese content of the water.

The raw water obtained from 100 different wells will be purified by a water treatment plant of 150,000 m³/day capacity. Considering the high iron content (0.05–0.15 mg/L) and manganese content (0.05–0.2 mg/L), the raw water fails to comply with the requirements of the potable water standard.

Since 1990, over a period of three years, we conducted water purification experiments in several stages. In these, three methods of oxidizing as well as single and double layer open rapid filters were applied to oxidize the manganese (and, to a lesser extent, the water) present in dissolved form, resp., to destroy various living organisms.

In the course of the experiments, it became clear that the chlorine and chlorine + air methods are efficient in case of a small quantity of iron to be oxidized and only 20–25% of the dissolved manganese content could be oxidized.

Neither of the two methods could ensure firm management of microbiological and bacteriological characteristics. The best results were obtained by ozone oxidation, in which case the chemical oxidizing process was almost fully completed and even the chlorine-resistant living organisms could be destroyed.

On the basis of the experiments carried out, the investment program of the water treatment plant was worked out and the conditions of an international tender were compiled whose winner will be commissioned to build up the water works in the time period 1993–1996. One of the main steps of the proposed technology is the ozone treatment.     

Magneto-Inertial Fusion

In this community white paper, we describe an approach to achieving fusion which employs a hybrid of elements from the traditional magnetic and inertial fusion concepts, called magneto-inertial fusion (MIF). The status of MIF research in North America at multiple institutions is summarized including recent progress, research opportunities, and future plans.     

Corrosion behaviour of as-cast ZK40 with CaO and Y additions

The microstructures of as-cast ZK40, ZK40 with 2% (mass fraction) CaO and ZK40 with 1% (mass fraction) Y were investigated, and the intermetallic phase morphology and the distribution were characterised. By having discrete intermetallic particles at the grain boundaries for the ZK40, the microstructure was modified to a semi-continuous network of intermetallic compounds along the grain boundaries for the ZK40 with CaO or Y additions. The CaO was not found in the microstructure. However, Ca was present in Ca₂Mg₆Zn₃ intermetallic compounds which were formed during casting. Hydrogen evolution and electrochemical impedance spectroscopy tests revealed that the addition of CaO slightly enhanced the corrosion resistance whereas Y had a negative effect on the corrosion resistance of ZK40. Immersion tests showed that severe localised corrosion as well as corrosion along the intermetallic compounds played an important role in the corrosion process of ZK40–Y whereas the localised corrosion was not pronounced for ZK40 or ZK40–CaO alloys. Micro-segregation in the α-Mg matrix was notably higher for the ZK40 alloy compared with the modified alloys. The combination of this effect with a possible formation of a more stable corrosion layer for the ZK40–CaO was attributed as the main reason for an improved corrosion resistance for the ZK40–CaO alloy.     

Flame retardants in building insulation: a case for re-evaluating building codes

US building codes balance the consideration of hazards to public safety, health and general welfare. Current codes require foam plastic insulation materials to have both protection by a thermal barrier and compliance with Steiner Tunnel test requirements. The Steiner Tunnel test is met by adding flame-retardant chemicals to the foam. Studies demonstrate that the Steiner Tunnel test does not give reliable fire safety results for foam plastic insulations. Foams that meet the Steiner Tunnel test still pose a fire hazard if used without a code-mandated thermal barrier. Insulations protected by a thermal barrier are fire safe and the use of flame retardants does not provide any additional benefit. Evidence is examined of the health and ecological impacts from the added flame-retardant chemicals. Changing the building codes could prevent health and environmental harm from the toxicity of these substances without a reduction in fire safety. Plastic foam insulations that are protected by a thermal barrier should be exempted from the Steiner Tunnel test and the need to use flame retardants. This change would align US codes with code regulations in Sweden and Norway and ensure the fire safety as well as improve health and environmental impacts.

Les codes de construction américains prennent en compte de manière équilibrée les dangers pour la sécurité publique, la santé et le bien-être général. Les codes actuels exigent que les matériaux d'isolation en mousse de plastique possèdent à la fois une protection assurée par une barrière thermique et une conformité aux exigences des tests en tunnel Steiner. Il est satisfait à l'essai en tunnel Steiner par l'ajout à la mousse de produits chimiques retardateurs de flamme. Les études démontrent que l'essai en tunnel Steiner ne donne pas de résultats fiables en matière de sécurité incendie concernant les isolations en mousse de plastique. Les mousses qui satisfont à cet essai présentent encore un risque incendie en cas d'utilisation sans une barrière thermique prescrite par un code. Les isolations protégées par une barrière thermique sont ignifuges et l'utilisation de retardateurs de flamme n'apporte aucun avantage supplémentaire. Sont examinés les éléments probants relatifs aux incidences sur la santé et l'environnement des produits chimiques retardateurs de flamme qui sont ajoutés. La modification des codes de construction pourrait prévenir les dommages en matière de santé et d'environnement dus à la toxicité de ces substances sans réduction de la sécurité incendie. Les isolations en mousse de plastique qui sont protégées par une barrière thermique devraient être dispensées de l'essai en tunnel Steiner et de la nécessité d'utiliser des retardateurs de flamme. Ce changement alignerait les codes américains sur les règles des codes en vigueur en Suède et en Norvège et garantirait la sécurité incendie tout en améliorant les incidences sur la santé et l'environnement.

Mots clés: codes de construction?sécurité incendie?retardateurs de flamme?inflammabilité?isolation?santé publique?Tunnel Steiner?barrière thermique?toxicité     

Polymer‐based nucleation for chemical vapour deposition of diamond

Chemical vapour deposition of diamond on foreign substrates is hindered due to its high surface energy. Therefore, nucleation treatment has to be employed to initialize the formation of diamond crystals. This article deals with diamond growth on silicon substrates coated with three types of polymers: (i) polystyrene (PS), (ii) polylactic‐co‐glycolic acid (PLGA), and (iii) polyvinyl alcohol (PVA) were applied in different forms, i.e., microspheres (PS, PLGA), monolayers (PLGA), multilayers (PLGA, PLGA/PS), and composites with embedded diamond nanoparticles (PLGA, PVA). Thin polymers and microsphere monolayers did not contribute to the diamond nucleation and/or growth. A thicker continuous polymer film (>750 nm) or thin polymer/microsphere layer led to a homogeneous and dense formation of diamond grains. In the case of nucleation using polymer composites, where the thin polymer film serves as a 3D carrier matrix for embedded diamond nanoparticles, a comparable nucleation density to the well‐established ultrasonic seeding method was achieved. © 2016 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133, 43688.