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.     

Investigation of thermal residual stresses during laser ablation of tantalum carbide coated graphite substrates using micro-Raman spectroscopy and COMSOL multiphysics

Laser ablation of high-temperature ceramic coatings results in thermal residual stresses due to which the coatings fail by cracking and debonding. Hence, the measurement of such residual stresses during laser ablation process holds utmost importance from the view of performance of coatings in extreme conditions. The present research aims at investigating the effect of laser parameters such as laser pulse energy, scanning speed and line spacing on thermal residual stresses induced in tantalum carbide-coated graphite substrates. Residual stresses were measured using micro-Raman spectroscopy and correlated with Raman peak shifts. Transient thermal analysis was performed using COMSOL Multiphysics to model the single ablated track and residual stresses were reported at low, moderate and high pulse energy regimes. The results showed that the initial laser conditions caused higher tensile residual stresses. Moderate pulse energy regime comprised higher compressive residual stresses due to off centre overlapping of the laser pulses. Higher pulse energy (250 μJ), higher scanning speed (1000 mm/s) and moderate line spacing (20 μm) caused accumulation of tensile residual stresses during the final stage of laser ablation. The deviation of experimental residual stresses from COMSOL numerical model was attributed to unaccounted additional stresses induced during thermal spraying process and deformation potentials in the numerical model.     

Evaluating the Possibility of Using Ionic Liquids in the Synthesis and Separation of Cyclohexanone

Theoretical Foundations of Chemical Engineering - Using gas–liquid chromatography, the activity coefficients upon the infinite dilution of the components of the reaction mixture for obtaining...     

Segmental Baffles as a Means of Improving the Heat Transfer Efficiency of Air Coolers

Chemical and Petroleum Engineering - A comparative analysis of the main types of air coolers (ACs) is presented. Their advantages and disadvantages are indicated along with the main approaches for...     

Environmental effects on the strength and impact damage resistance of alumina based oxide/oxide ceramic matrix composites

In this study the effects of high temperature and moisture on the impact damage resistance and mechanical strength of Nextel 610/alumina silicate ceramic matrix composites were experimentally evaluated. Composite laminates were exposed to either a 1050°C isothermal furnace-based environment for 30 consecutive days at 6 h a day, or 95% relative humidity environment for 13 consecutive days at 67°C. Low velocity impact, tensile and short beam strength tests were performed on both ambient and environmentally conditioned laminates and damage was characterized using a combination of non-destructive and destructive techniques. High temperature and humidity environmental exposure adversely affected the impact resistance of the composite laminates. For all the environments, planar internal damage area was greater than the back side dent area, which in turn was greater than the impactor side dent area. Evidence of environmental embrittlement through a stiffer tensile response was noted for the high temperature exposed laminates while the short beam strength tests showed greater propensity for interlaminar shear failure in the moisture exposed laminates. Destructive evaluations exposed larger, more pronounced delaminations in the environmentally conditioned laminates in comparison to the ambient ones. External damage metrics of the impactor side dent depth and area directly influenced the post-impact tensile strength of the laminates while no such trend between internal damage area and residual strength could be ascertained.     

Enhancement of glass-ceramic performance by TiO2 doping: In vitro cell viability,proliferation, and differentiation

A new TiO₂-containing bioactive glass and glass-ceramics based on 50SiO₂-(45-X)CaO-(XTiO₂)-5P₂O₅ system was designed using a sol–gel technique (where X = 5, 7.5 and 10 wt %). The roles of the crystallization behavior and physicochemical characteristics of the designed glass and glass-ceramics which were played in the introduction of TiO₂ substitutions were investigated. Moreover, cell proliferation and differentiation were evaluated against human osteosarcoma cells (Saos-2). The TiO₂/CaO replacements led to the formation of a stronger glass structure and thus increased thermal parameters and the chemical stabilization of the designed materials. The FTIR data confirmed the existence of Ti within the glass and glass-ceramics samples, and no remarkable effect on their chemical integrity was observed. The XRD patterns indicated that calcium-containing minerals, including Ca₂SiO₄,Ca₃(PO₄)₂, Ca(Ti,Si)O₅, CaTiSiO₅, and Ca₁₅(PO₄)₂·(SiO₄)₆ phases were developed as a role of structure/texture under the applied heat-treatment. The results of the cytotoxicity test proved that a safe sample dose is 12–50 μg/ml, at which cell viability is ≥ 85%. The cell differentiation determined by ALP test proved the superiority of glass-ceramics compared with their native glasses. Therefore, the obtained materials could be safely used as novel biocompatible materials for the regeneration of bone tissue.     

Influence of pH on the DSSC Performance of Template Assisted SnO2 Nanostructures

Journal of Inorganic and Organometallic Polymers and Materials - This paper reports the performance of alizarin based SnO2 dye-sensitized solar cells. A novel template assisted method has been...     

Quantum-Confinement Effect in Silicon Nanocrystals during Their Dissolution in Model Biological Fluids

Semiconductors - In present work, we studied the mechanisms of dissolution of porous silicon nanoparticles (PSi NPs) during their incubation in model liquids, i.e. water and phosphate buffered...     

Optimizing Approach of Water Allocation to Off-Takes During Reduced Flows

Multi-objective optimization models with an index were developed based on farmers’ preferences, local requirements, supplies available at the head of the canal, system losses, crop demand about different growth stages, and field soil moisture balance. The models were applied using linear programming. The Model 1 determines the cropping pattern by maximizing net economic benefits using a monthly basis lumped volume available at the head of the canal and is set to the minimum and maximum area constraints along with the constraint of minimum main crop area. The areas for different crops given by the first model form input for the Model 2. The other inputs of Model 2 included periodic supply available at the head of the primary canal (7-day period in this study), root growth depth, demand, and soil moisture constants. The Model 2 optimizes the sum of relative yields of all the crops and provide the irrigation levels of various crops for specified periods. Finally, the distributed area and irrigation levels determined by Model 2 are used in conjunction with the losses to decide flow rates of off takes. The complete program was implemented in the West branch irrigated area of Mirpurkhas subdivision. The results showed that the resources were allocated to off-takes in a competitive and conflict-free manner.