Pd‐Mediated Multicomponent Synthesis of Highly Functionalized Pyridines and Consequential C—C Coupling Using Suzuki Reaction in One Pot: Their In Vitro Evaluation as Potential Antibacterial Agents

Pd‐mediated construction of pyridine scaffold and subsequent Suzuki‐based C—C coupling reaction in one pot has been accomplished for the synthesis of 4‐biaryl substituted 2‐amino‐3‐cyanopyridines via multicomponent reaction. The present multicomponent reaction is useful in structural elaboration of pyridine framework and also helpful in design and synthesis of novel and diverse analogs of complex heterocyclic compounds other than present reported molecules. Antibacterial activities of the synthesized compounds were systematically evaluated. The correlation between functional group variation and biological activities of the compounds has been evaluated against human pathogenic gram‐positive and gram‐negative bacterial strains.     

A Facile Route for the Synthesis of Novel Heterocyclic Prostaglandin F2α Analogs

A general synthetic approach has been developed for heterocyclic prostaglandins (PGF_2α type) starting from the key intermediate ( 6 ). (±) 6 was obtained from (±) ‐Corey lactone. The key intermediate (±) 6 was, in turn, converted in to several new heterocyclic prostaglandins consisting of furan and thiophene moieties in ω‐side chain in two to three steps. Horner–Wadsworth–Emmons reaction and Grignard reaction as the key reactions in these transformations.     

Hepatoprotective Effect of β-Chitosan from Gladius of Sepioteuthis lessoniana Against Carbon Tetrachloride-Induced Oxidative Stress in Wistar Rats

Chitosan has attracted much attention as a biomedical material, owing to its unique biological activities. In this study, hepatoprotective effect of β-chitosan obtained from the gladius of squid Sepioteuthis lessoniana was studied against carbon tetrachloride (CCl₄)-induced oxidative stress and liver injury in rats. The rats that received β-chitosan along with the administration of CCl₄ showed significantly decreased plasma and tissue alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities and total cholesterol, triglyceride (TG) and free fatty acid (FFA) contents, whereas the treatment with β-chitosan alone markedly increased rat hepatic and circulatory superoxide dismutase (SOD), catalase and glutathione peroxidase (GPx) and reduced glutathione (GSH) levels and decreased the malondialdehyde level. Histopathological observations recommended the marked hepatoprotective effect of β-chitosan. The CCl₄-induced alterations on circulatory and hepatic antioxidant defence system were normalised by β-chitosan, and it could be concluded that the hepatoprotective effect of chitosan may be due to its antioxidant and antilipidemic property. Therefore, β-chitosan could be considered as antihepatotoxic agent.     

Square Planar Platinum(II) Complexes with N,S-Donor Ligands: Synthesis,Characterisation, DNA Interaction and Cytotoxic Activity

The platinum(II) complexes with N,S-donor ligand have been synthesised and characterised by physiological techniques like elemental, electronic, Fourier transform infrared, hydrogen-1 nuclear magnetic resonance (¹H NMR) and liquid chromatography–mass spectrometry spectra. The synthesised complexes have been checked for their DNA binding ability by absorption titration and viscosity measurement, and the results show that the complexes binds to herring sperm DNA (HS DNA) via covalent mode of binding. The DNA cleavage activity of synthesised complexes has been carried out by gel electrophoresis experiment using supercoiled form of pUC19 DNA, showing the unwinding of the negatively charged supercoiled DNA. Brine shrimp (Artemia cysts) lethality bioassay technique has been applied for the determination of toxic property of synthesised complexes in terms of micromolars.     

Some results on λ‐designs with two block sizes

A λ‐design is a family ?? = {B₁, B₂, …, B_v} of subsets of X = {1, 2, …, v} such that |B_i∩B_j| = λ for all i≠jand not all B_i are of the same size. The only known example of λ‐designs (called type‐1 designs) are those obtained from symmetric designs by a certain complementation procedure. Ryser [J Algebra 10 (1968), 246–261] and Woodall [Proc London Math Soc 20 (1970), 669–687] independently conjectured that all λ‐designs are type‐1. Let g = gcd(r ? 1, r^* ? 1), where rand r^* are the two replication numbers. Ionin and Shrikhande [J Combin Comput 22 (1996), 135–142; J Combin Theory Ser A 74 (1996), 100–114] showed that λ‐designs with g = 1, 2, 3, 4 are type‐1 and that the Ryser–Woodall conjecture is true for λ‐designs on p + 1, 2p + 1, 3p + 1, 4p + 1 points, where pis a prime. Hein and Ionin [Codes and Designs—Proceedings of Conference honoring Prof. D. K. Ray‐Chaudhuri on the occasion of his 65th birthday, Ohio State University Mathematical Research Institute Publications, 10, Walter de Gruyter, Berlin, 2002, pp. 145–156] proved corresponding results for g = 5 and Fiala [Codes and Designs—Proceedings of Conference honoring Prof. D. K. Ray‐Chaudhuri on the occasion of his 65th birthday, Ohio State University Mathematical Research Institute Publications, 10, Walter de Gruyter, Berlin, 2002, pp. 109–124; Ars Combin 68 (2003), 17–32; Ars Combin, to appear] for g = 6, 7, and 8. In this article, we consider λ designs with exactly two block sizes. We show that in this case, the conjecture is true for g = 9, 11, 12, 13, 15, 16, 17, 19, 20, 21, and for g = 10, 14, 18, 22 with v≠4λ ? 1. We also give two results on such λ‐designs on v = 9p + 1 and 12p + 1 points, where pis a prime. © 2010 Wiley Periodicals, Inc. J Combin Designs 19:95‐110, 2011     

Do Two Flavour Oscillations Explain both KamLAND Data and the Solar Neutrino Spectrum?

The recent measurement of Δ _sol by the KamLAND experiment with very small errors, makes definitive predictions for the energy dependence of the solar neutrino survival probability P _ee . We fix Δ _sol to be the KamLAND best fit value of 8×10⁻⁵ eV² and study the energy dependence of P _ee for solar neutrinos, in the framework of two flavour oscillations and also of three flavour oscillations. For the case of two flavour oscillations, P _ee has a measurable slope in the 5–8 MeV range but the solar spectrum measurements in this range find P _ee to be flat. The predicted values of P _ee , even for the best fit value of θ _sol , differ by 2–3 σ from the Super-K measured values in each of the three energy bins of the 5–8 MeV range. If future measurements of solar neutrinos by Super-K and SNO find a flat spectrum with reduced error bars (by a factor of 2), it will imply that two flavour oscillations can no longer explain both KamLAND data and the solar spectrum. However a flat solar neutrino spectrum and the Δ _sol measured by KamLAND can be reconciled in a three flavour oscillation framework with a moderate value of θ ₁₃≈13°.     

Halide Anion Triggered Reactions of Michael Acceptors with Tropylium Ion

Tropylium bromide undergoes noncatalyzed, regioselective additions to a large variety of Michael acceptors. In this way, acrylic esters are converted into β‐bromo‐α‐cycloheptatrienylpropionic esters. The reactions are interpreted as nucleophilic attack of bromide ions at the electron‐deficient olefins and the approach of the tropylium ion to the incipient carbanion. Quantum chemical calculations were performed to elucidate the analogy to the amine‐ or phosphine‐catalyzed Rauhut–Currier reactions. Subsequent synthetic transformations of the bromo‐cycloheptatrienylated adducts are reported.     

Fabrication and characterization of a novel wound scaffold based on polyurethane added with Channa striatus for wound dressing applications

Abstract

Wound healing is a complex process and it involves restoration of damaged skin tissues. Several wound dressings comprising naturally made substances are constantly investigated to assist wound healing. In this research, a new wound dressing based on polyurethane (PU) supplemented with essence of Channa striatus (CS) fish oil was made by electrospinning. Morphological study depicted the reduction in fiber diameter than PU with the addition of fish oil (0.552?±?0.109?μm for 8:1 v/v% and 0.519?±?0.196?μm 7:2 v/v%) than the pristine PU (0.971?±?0.205?µm). Fourier transform infrared spectroscopy (FTIR) analysis revealed the presence of fish oil in the composite as identified through increasing peak intensity. Fish oil resulted in the hydrophilic behavior (88?±?3 (8:1 v/v) and 70?±?6 (7:2 v/v)) as revealed in the contact angle analysis. Thermal gravimetric analysis (TGA) showed the superior thermal behavior of the wound dressing patch compared to the PU. Atomic force microscopy (AFM) analysis insinuated a decrease in the surface roughness of the pristine polyurethane with the added fish oil. Coagulation assays signified the delay in the blood clotting time portraying its anti-thrombogenic behavior. Hemolytic assay revealed the less toxic nature of the developed nanocomposites with the red blood cells (RBC’s) depicting its safety with blood. Hence, polyurethane nanofibers supplemented with fish oil made them as deserving candidates for wound dressing application.     

Influence of sputter power on structural and electrical properties of TiO2 films for Al/TiO2/Si gate capacitors

Titanium dioxide (TiO₂) thin films were deposited onto p‐Si substrates held at room temperature by reactive Direct Current (DC) magnetron sputtering at various sputter powers in the range 80–200 W. The as‐deposited TiO₂ films were annealed at a temperature of 1023 K. The post‐annealed films were characterized for crystallographic structure, chemical binding configuration, surface morphology and optical absorption. The electrical and dielectric properties of Al/TiO₂/p‐Si structure were determined from the capacitance–voltage and current–voltage characteristics. X‐ray diffraction studies confirmed that the as‐deposited films were amorphous in nature. After post‐annealing at 1023 K, the films formed at lower powers exhibited anatase phase, where as those deposited at sputter powers > 160 W showed the mixed anatase and rutile phases of TiO₂. The surface morphology of the films varied significantly with the increase of sputter power. The electrical and dielectric properties on the air‐annealed Al/TiO₂/p‐Si structures were studied. The effect of sputter power on the electrical and dielectric characteristics of the structure of Al/TiO₂/p‐Si (metal‐insulator‐semiconductor) was systematically investigated. Copyright © 2014 John Wiley & Sons, Ltd.     

Comparative Study of Catalytic Potential of TBAB,BTEAC, and CTAB in One-Pot Synthesis of 1,4-Dihydropyridines Under Aqueous Medium

Convenient and straightforward tetrabutylammonium bromide (TBAB), benzyltrienthylammonium chloride (BTEAC), and cetyltrimethylammonium bromide (CTAB) catalyzed synthesis of 1,4-dihydropyridines (1,4-DHPs) in water was established for the first time. The catalytic potential of phase-transfer catalysts (PTCs) in three different concentrations was envisioned. Aryl aldehydes and hetero aryl aldehydes afforded good yields of 1,4-DHPs in TBAB and BTEAC reactions. In particular, furfuraldehyde and thienyl-2-carbaldehyde produced excellent yields. Isolation of the products through nonchromatographic methods, good to excellent yields, and benign reaction conditions are the major advantages of this protocol.