1-[2-(1-Cyclobutylpiperidin-4-yloxy)-6,7-dihydro-4H-thiazolo[5,4-c]pyridin-5-yl]propan-1-one: a Histamine H3 Receptor Inverse Agonist with Efficacy in Animal Models of Cognition

A series of chemical optimizations, which was guided by in vitro affinity at histamine H₃ receptor (H₃R), modulation of lipophilicity, ADME properties and preclinical efficacy resulted in the identification of 1-[2-(1-cyclobutylpiperidin-4-yloxy)-6,7-dihydro-4H-thiazolo[5,4-c]pyridin-5-yl]propan-1-one ( 45 e ) as a potent and selective (K_i=4.0 nM) H₃R inverse agonist. Dipsogenia induced by (R)-α-methylhistamine was dose dependently antagonized by 45 e , confirming its functional antagonism at H₃R. It is devoid of hERG and phospholipidosis issues. Compound 45 e has adequate oral exposures and favorable half-life in both rats and dogs. It has demonstrated high receptor occupancy (ED₈₀=0.22 mg/kg) and robust efficacy in object recognition task and, dose dependently increased acetylcholine levels in brain. The sub-therapeutic doses of 45 e in combination with donepezil significantly increased acetylcholine levels. The potent affinity, selectivity, in vivo efficacy and drug like properties together with safety, warrant for further development of this molecule for potential treatment of cognitive disorders associated with Alzheimer's disease.     

Electrochemical synthesis and characterization of poly(aniline-co-1-amino-9,10-anthraquinone), a nanosized conducting copolymer

The electrochemical copolymerization of aniline (ANI) with 1-amino-9,10-anthraquinone (1-AAQ) was carried out in 4 M sulfuric acid by potential cycling in the potential range of −0.1 V to 1.3 V vs. SCE. Copolymer films were grown from different feed ratios of ANI and 1-AAQ (0.2:0.8, 0.4:0.6, 0.5:0.5, 0.6:0.4, 0.8:0.2) on a glassy carbon electrode (GCE). Studies on the effect of scan rate on the conductivity of the copolymer film confirmed the formation of a stable conducting copolymer film. The FTIR spectrum recorded for the copolymer film provides concrete evidence of copolymer formation, since it indicates the presence of quinone units in the copolymer backbone. XRD data (particle size: 47 nm) and SEM (grain size: 100 nm) micrographs provide a clear picture of the nano-sized polymeric particles formed. It is envisaged that the newly reported copolymer could be a useful material for performing the catalytic reduction of oxygen in an acidic medium—a useful process for fuel cell applications.     

Phthalocyanine- and Calixarene-Templating Effect on the Catalytic Performance of Solid Supported Vanadates

Abstract  

Catalytic performance of solid supported monovanadate catalysts toward oxidation of propane is significantly affected by the templating effect of: (1) pretreatment of the solid support with calixarene derivatives before deposition of ammonium vanadate, (2) direct deposition of vanadyl phthalocyanine as the vanadate precursor. This effect is believed to be linked to the accessibility of the active sites, and was studied in comparison with a reference mesoporous support.     

Structural and electrochemical impedance spectroscopic studies on reactive magnetron sputtered titanium oxynitride (TiON) thin films

Titanium oxynitride films were deposited onto commercially pure titanium substrates by direct current reactive magnetron sputtering method using Ti targets and an Ar–N₂–O₂ mixture discharge gas. The X-ray photoelectron spectroscopy survey spectra on the etched surfaces of TiON films exhibited the characteristic Ti 2p, N 1s, and O 1s peaks at the corresponding binding energies 454.5, 397.0, and 530.7 eV, respectively. The surface topography of these coatings was studied using atomic force microscopy. The characteristic Raman peaks at 200 and 641 cm⁻¹ for the TiN bonds and at 148, 398 ,and 518 cm⁻¹ for the TiO₂ bonds were observed from the Laser Raman spectrometer. The potentiodynamic polarization studies in simulated bodily fluid were performed and the results are reported in this article.     

Applications of wittig reactions in dibenzo 18‐crown‐6‐ether substituted phenylenevinylene oligomer—synthesis,photo luminescent,and dielectric properties

Novel phenylenevinylene oligomer substituted dibenzo 18‐crown‐6 ether ring (DB‐OPV) was synthesized using dibenzo 18‐crown‐6 with terephthaldicarboxaldehyde via Wittig reaction. Formation of the oligomer was confirmed by spectral (FT‐IR, ¹H and¹³C‐NMR), gel‐permeation chromatography and elemental analysis. The morphology of the oligomer film of one‐dimensional and three‐dimensional architectures was observed using atomic force microscopy. The oligomer showed excellent photoluminescence with bluish green emission maxima at shorter wavelengths of 505 nm. Stability of the oligomer was analyzed using UV spectroscopy with varying time and temperature. The dielectric properties such as dielectric constant and loss factor for the oligomer have also been studied with respect to change of frequency (50 Hz–5 MHz) and temperature (30–60°C). The value of dielectric constant decreased with increasing frequency, which indicates that the major contribution to the polarization comes from orientation polarization. The value of dielectric constant increased with increasing temperature which is due to greater freedom of movement of the dipole molecular chains within the oligomer at high temperature © 2010 Wiley Periodicals, Inc. J Appl Polym Sci, 2011     

Separation of oil constituents in organic solvents using polymeric membranes

Different types of commercial nonporous (reverse osmosis and gas separation) polymeric membranes were screened for their abilities to separate FFA, MG, DG, and TG from a lipase hydrolysate of high-oleic sunflower oil after diluting it with organic solvents (ethanol and hexane). Cellulose acetate (CA) (NIR-1698) membrane gave the largest difference in rejection between FFA and glycerides and high flux in oil/ethanol mixtures. In the hexane system, the values of permeate flux and rejection were generally lower than those in the ethanol system. The silicone-polyimide composite membrane (NTGS-2100) gave the highest flux and rejections of solutes (70.2% for FFA, 94.4% for TG) in oil/hexane mixtures. In the ethanol system with the CA membrane, TG had the highest rejection (98%) followed by DG (90%) and MG and FFA (50–70%) when the oil concentration was varied from 6.3 to 45.8%. A discontinuous diafiltration process (16 batches) using the CA membrane with ethanol changed the composition of the oil from 31∶28∶9∶32 TG/DG/MG/FFA to 65∶30∶1∶4. The results of this study showed that oil constituents can be separated in suitable solvents using appropriate nonporous membranes.     

Coumarin‐based polymer and its silver nanocomposite as advanced antibacterial agents: Synthetic path,kinetics of polymerization,and applications

A novel polymer bearing coumarin pendants of 4‐allyloxy‐2H‐chromen‐2‐one (ACO) was synthesized by atom transfer radical polymerization (ATRP) in toluene at 110°C using 2‐Bromoisobutyryl bromide (BIBB), Cu (I) Br, and 2,2′‐bipyridyl (bpy) as initiator, catalyst, and ligand, respectively. The most appropriate molar concentration ratio of [ACO] : [BIBB] : [Cu (I) Br] : [bpy] was found to be 40 : 1 : 1 : 2 for controlled polymerization. Successful chain extension polymerization of poly (4‐allyloxy‐2H‐chromen‐2‐one) (PACO) confirms the livingness of the process. The activation energy (E_a) (76.26 kJ mol^?1) and enthalpy of activation (ΔH^?) (73.07 kJ mol^?1) were in good agreement to each other proving the feasibility of the reaction and negative value of entropy of activation (ΔS^?) (?320 J mol^?1 K^?1) supported the highly restricted movement of reacting species in transition state during polymerization. Initial polymer decomposition temperature of PACO was found to be 130°C. SEM analysis revealed that polymer surface is not smooth with pointed rod like shapes. The polymer/Ag nanocomposite was synthesized and examined in view of antibacterial effect against Enterococcus faecalis, Staphylococcus aureus, Escherichia coli, Proteus mirabilis, and Klebsiella pneumonae. PACO and its Ag nanocomposite (PACON) have been found to be active selectively against bacterial pathogen E. fecalis with minimum inhibitory concentration of 50 and 32 μg mL^?1, respectively. © 2012 Wiley Periodicals, Inc. J Appl Polym Sci, 2012     

Mechanochemical synthesis and characterization of poly(2,5‐dimethoxy aniline) salts

The interfacial interaction and orientation of molecules during the polymerization process plays a vital role in the enhancement of the surface properties of conducting polymers. In this perspective, a solid‐phase mechanochemical route is employed to prepare poly(2,5‐dimethoxy aniline) (PDMA) and its salts with superior properties. Various studies performed on the as‐prepared polymer highlights the formation of polymeric particles with excellent physicochemical properties. Elemental analysis showed the presence of dopants anion in the polymeric backbone. Spectroscopic profile of PDMAs revealed the formation of emeraldine form of PDMAs. Moreover, these studies indicate the formation of PDMA‐HCl in a highly doped state. The surface morphological pictures of PDMAs revealed the formation of aggregated microstructured to nanostructured particulates. X‐ray diffraction, cyclic voltammetry were used to evaluate the physicochemical properties of PDMAs. PDMA salts exhibited crystalline behavior and good electrochemical activity. TG/DTA analysis showed that all the PDMAs were thermally stable up to 240°C. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2012     

Pd-Decorated Tungsten as Pt-Free Bimetallic Catalysts for Hydrogen Oxidation Reaction in Alkaline Electrolyte

Developing Pt-free catalysts for hydrogen oxidation reaction (HOR) in alkaline solution is becoming a key challenge in the development of anion exchange membrane fuel cells and electrochemical reactors. Herein, we present the preparation, HOR activity, and stability of Pd-decorated tungsten (Pd-d-W) catalysts. The Pd-d-W catalysts were prepared by the chemically activated surface of tungsten nanoparticles by Pd ions. The resultant bimetallic catalysts consisted of crystalline phases of both Pd and W nanoparticles. The CO stripping voltammograms and H-desorption (H_des) peak potential of hydrogen desorption in Pd suggests that the enhancement of HOR catalytic activity observed in Pd-d-W catalyst can be ascribed to the modification of electronic property of Pd and availability of OH_ad near-surface Pd atoms.     

Simultaneous accommodation of Dy3+ at the lattice site of β-Ca3(PO4)2 and t-ZrO2 mixtures: Structural stability,mechanical, optical,and magnetic features

Structurally stable β-Ca₃(PO₄)₂/t-ZrO₂ composite mixtures with the aid of Dy³⁺ stabilizer were accomplished at 1500°C. The precursors comprising Ca²⁺, P⁵⁺, Zr⁴⁺, and Dy³⁺ have been varied to obtain five different combinations. The results revealed the fact that complete phase transformation of calcium-deficient apatite to β-Ca₃(PO₄)₂ occurred only at 1300°C, whereas the evidence of t-ZrO₂ crystallization is obvious at 900°C. The dual occupancy of Dy³⁺ at β-Ca₃(PO₄)₂ and t-ZrO₂ structures was evident; however, Dy³⁺ initially prefers to occupy β-Ca₃(PO₄)₂ lattice until its saturation limit and thereafter accommodates at the lattice site of ZrO₂. The typical absorption and emission behavior of Dy³⁺ were noticed in all the systems and, moreover, the surrounding symmetry of Dy³⁺ domains has been determined from the luminescence study. All the systems ensured paramagnetic response that is generally contributed by the presence of Dy³⁺. A gradual increment in the phase content of t-ZrO₂ in the composite mixtures ensured a significant improvement in the hardness and Young's modulus of the investigated compositions.