Design and synthesis of an octavalent bolaamphiphile with terminal lactose residues

The synthesis of an octavalent bolaamphiphile with D-glucose moiety as branching unit has been designed and accomplished via 1,3-dipolar cycloaddition of bis(tetra-O-propargylglucoside) and 8 equiv of 2-azidoethyl β-D-lactoside.     

Acceleration of Acetal Hydrolysis by Remote Alkoxy Groups: Evidence for Electrostatic Effects on the Formation of Oxocarbenium Ions

In contrast to observations with carbohydrates, experiments with 4‐alkoxy‐substituted acetals indicate that an alkoxy group can accelerate acetal hydrolysis by up to 20‐fold compared to substrates without an alkoxy group. The acceleration of ionization in more flexible acetals can be up to 200‐fold when compensated for inductive effects.     

Direct Catalytic Enantio‐ and Diastereoselective Ketone Aldol Reactions of Isocyanoacetates

A catalytic asymmetric aldol addition/cyclization reaction of unactivated ketones with isocyanoacetate pronucleophiles has been developed. A quinine‐derived aminophosphine precatalyst and silver oxide were found to be an effective binary catalyst system and promoted the reaction to afford chiral oxazolines possessing a fully substituted stereocenter with good diastereoselectivities and excellent enantioselectivities.     

Improvements to CO<Subscript>2</Subscript> headspace biodegradability test

This study proposes changes to the design and evaluation of the CO₂ headspace test, which is used as a simple method for assessment of the complete biodegradability of surfactants. It presents a modified equation for the calculation of biodegradation. It is proposed that the solution of 7 mol L^?1 sodium hydroxide commonly used in the process involving alkalinisation of the vial contents be replaced with 15 mol L^?1 sodium hydroxide. The use of the higher hydroxide concentration leads to a significant reduction in the value of the blank CO₂ headspace test.     

Antioxidative properties of <Emphasis Type="Italic">Sambucus nigra</Emphasis> extracts

Potential protective effects of elderberry (Sambucus nigra) extracts against oxidative degradation of hyaluronan (HA) were detected in vitro. To induce free-radical-mediated HA degradation, Weissberger’s biogenic oxidative system, which mimics the situation of acute inflammation, was applied. Time- and dose-dependent changes of dynamic viscosity of the HA solutions in the presence and absence of two elderberry extracts produced in 2006 and 2012 were recorded by rotational viscometry (RV). Radical scavenging capacity of both extracts was investigated by the spectrocolorimetric ABTS [2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt] assay and the “inverted” ABTS assay. Oxygen consumption of the system oxidizing HA either in the absence or presence of the elderberry extracts was determined. The results of RV revealed that an addition of the newer extract (2012) promoted the inhibition of HA degradation more markedly compared to the older extract (2006). The same effect of both extracts on ABTS^·+ scavenging was observed. Inverted ABTS assay demonstrated that colorful substances were not responsible for the radical-scavenging activity. Results of oximetry demonstrated that the effect of the extract from 2006 was more significant than that of the extract from 2012.     

Determination of acid volatile sulphur in river sediments by ICP-OES coupled with purge and trap method

The developed and tested method is based on the acid volatile sulphur (AVS) releasing from a sample of sediment by acidification with hydrochloric acid and sequential absorption of released hydrogen sulphide into the absorption solution of sodium hydroxide. Total sulphur absorbed in the absorption solution is subsequently determined by inductively coupled plasma optical emission spectrometry (ICP-OES) technique. The method was tested using both model and real samples of the river sediment. Obtained results were compared with the results of iodometric determination as the method routinely used for the AVS determination. In case of using ICP-OES with purge and trap, there is no spectral interference of calcium; therefore for the determination of sulphur, it is possible to use atomic emission line of sulphur S I 180.7 nm. The tested method provides the results comparable with the iodometric method within the range of tested concentrations. The detection limit (LOD) of this method is 0.09 mg· S^2? ? L^?1 in the absorption solution which corresponds to 0.23 mg S^2?·kg^?1 in a sediment. Value of LOD is comparable with the iodometric determination.     

Synthesis and characterization of nano Ag end capped L-cysteine bridged diblock copolymer

The target of the present investigation is synthesis and characterization of an amphiphilic diblock copolymer with antibacterial property. Ring opening polymerization (ROP) of ε-caprolactone (CL) and tetrahydrofuran (THF) was carried out under inert atmosphere by using L-cysteine as a bridging agent in the presence of stannous octoate (SO) as a catalyst. The nano silver end capped diblock copolymer was synthesized by in situ method. Thus obtained nano silver end capped L-cysteine bridged diblock copolymer was characterized by various analytical methods like Fourier transform infrared (FTIR) spectroscopy, nuclear magnetic resonance (NMR) spectroscopy, circular dichroism (CD), fluorescence spectroscopy, gel permeation chromatography (GPC), X-ray photoelectron spectroscopy (XPS), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), field emission scanning electron microscopy (FESEM), high resolution transmission electron microscopy (HRTEM) and zeta potential. The antimicrobial property of the nano silver end capped diblock copolymer against e-coli was tested.     

Comparative theoretical study on the corrosion inhibition properties of benzoxazole and benzothiazole

Research on Chemical Intermediates - The electronic parameters of two azole molecules, namely benzoxazole (BOX) and benzothiazole (BTH), have been studied using DFT/B3LYP, MP2, and HF methods with...     

Selective Alkylation of C‐Rich Bulge Motifs in Nucleic Acids by Quinone Methide Derivatives

A quinone methide precursor featuring a bis‐cyclen anchoring moiety has been synthesized and its capacity to alkylate oligonucleotide targets quantified in the presence and absence of divalent metal ions (Zn²⁺, Ni²⁺ and Cd²⁺). The oligonucleotides were designed for testing the sequence and secondary structure specificity of the reaction. Gel electrophoretic analysis revealed predominant alkylation of C‐rich bulges, regardless of the presence of divalent metal ions or even the bis‐cyclen anchor. This C‐selectivity appears to be an intrinsic property of the quinone methide electrophile as reflected by its reaction with an equimolar mixture of the 2′‐deoxynucleosides. Only dA‐N1 and dC‐N3 alkylation products were detected initially and only the dC adduct persisted for detection under conditions of the gel electrophoretic analysis.     

Light‐Controlled Histone Deacetylase (HDAC) Inhibitors: Towards Photopharmacological Chemotherapy

Cancer treatment suffers from limitations that have a major impact on the patient’s quality of life and survival. In the case of chemotherapy, the systemic distribution of cytotoxic drugs reduces their efficacy and causes severe side effects due to nonselective toxicity. Photopharmacology allows a novel approach to address these problems because it employs external, local activation of chemotherapeutic agents by using light. The development of photoswitchable histone deacetylase (HDAC) inhibitors as potential antitumor agents is reported herein. Analogues of the clinically used chemotherapeutic agents vorinostat, panobinostat, and belinostat were designed with a photoswitchable azobenzene moiety incorporated into their structure. The most promising compound exhibits high inhibitory potency in the thermodynamically less stable cis form and a significantly lower activity for the trans form, both in terms of HDAC activity and proliferation of HeLa cells. This approach offers a clear prospect towards local photoactivation of HDAC inhibition to avoid severe side effects in chemotherapy.