Synthesis via direct (hetero)arylation polymerization, electrochemical and optical properties of poly (3,4-disubstituted)thiophenes

Some poly (3,4-disubstituted)thiophenes bearing both cyano and alkoxy or thioalkoxy groups have been synthesized by direct (hetero)arylation polymerization (DHAP) of 2-iodo-3,4-disubstituted thiophenes. The electron donor and acceptor properties of substituents in positions 3 and 4 allow to adjust the HOMO and LUMO levels. On the other hand, in order to avoid the polymer solubility problems, long branched or unbranched alkyl chains have also been introduced. Thus polymers with alkoxy groups have led to complete absorption in the wavelength range of the visible spectrum whereas in the presence of thioalkoxy groups, the absorption of the visible spectrum is only partial. Theoretical calculations have shown that sulphur creates torsions leading to a non-planar polymer chain

Small D-pi-A Systems with o-Phenylene-Bridged Accepting Units as Active Materials for Organic Photovoltaics

Donor-acceptor (D--A) systems that combine triarylamine donor blocks and dicyanovinyl (DCV) acceptor groups have been synthesized. Starting from the triphenylamine (TPA)thiopheneDCV compound (1) as a reference system, various synthetic approaches have been developed for controlling the light-harvesting properties and energy levels of the frontier orbitals in this molecule. Thus, the introduction of methoxy groups onto TPA, the replacement of one phenyl ring of TPA by a thiophene ring, or the extension of the -conjugating spacer group lead to the modulation of the HOMO level. On the other hand, the fusion of the DCV group onto the vicinal thiophene ring by an ortho-phenylene bridge allows for a specific fine-tuning of the LUMO level. The electronic properties of the molecules were analyzed by using UV/Vis spectroscopy and cyclic voltammetry and the compounds were evaluated as donor materials in basic bilayer planar heterojunction solar cells by using C-60 as acceptor material. The relationships between the electronic properties of the donors and the performance of the corresponding photovoltaic devices are discussed. Bilayer planar heterojunction solar cells that used reference compound 1 and C-70 afforded power-conversion efficiencies of up to 3.7%

Les effets pro-arythmiques des médicaments

RésuméLes effets pro-arythmiques des médicaments sont fréquents et graves, et sont associés à une surmortalité non négligeable. La polymédication augmente le nombre d’effets indésirables et d’interactions graves voire mortelles. Certains sont facilement évitables. Cependant, au-delà de l’allongement de l’intervalle QT, d’autres mécanismes peuvent avoir un rôle majeur comme les dysfonctions du RyR2, responsable d’arythmie calcium-dépendantes par surcharge calcique intracellulaire, avec apparition de post-dépolarisations tardives, sans modifications de l’intervalle QT. Les bloqueurs des canaux sodiques sont également un problème sérieux de part le risque de démasquer ou d’aggraver une dysfonction du canal sodique chez des patients atteints de syndrome de Brugada asymptomatique ou non. Leur dépistage à un stade précoce du développement des médicaments peut avoir un intérêt majeur.SummaryThe cardiac safety of new and marketed drugs is a major concern for public authorities, patients, physicians as well as pharmaceutical companies. Letal adverse drug reactions are indeed a leading cause of death worldwide and increase at a greater rate than the increase in total hospital admission. The increasing use of polypharmacy in current clinical practice is also associated to a growing number of side effects and interactions leading to fatal adverse events. Measurement of the QT interval is an established, albeit incomplete, approach to assess the proarrhythmic risk of a drug. Ventricular arrhythmia (VA) can be caused by a QT-prolonging drug inducing abnormal repolarization of the action potential (AP) of ventricular cardiomyocytes. Emerging evidence, derived from recent understanding of these mechanisms and of similar mechanisms reported for heart failure (HF), suggest that diastolic Ca2+ leak from the sarcoplasmic reticulum (SR) related to RyR2 dysfunction can induce Ca2+ dependent arrhythmia. In this report, we review mechanisms underlying drug-induced arrhythmogenic effects and Ca2+ dependent arrhythmia, and, for the latter, we discuss some of the issues associated to worsening of cardiac arrhythmias

Clean and Efficient Iodination of Thiophene Derivatives

Iodination of thiophene derivatives is realized using a simple, fast, and efficient methodology. Iodination of thiophene and 2- or 3-substituted or 3,4-disubstituted thiophenes with N-iodosuccinimide (NIS) activated with 4-toluenesulfonic acid in ethanol gives pure iodinated products that require no further purification

Opipramol inhibits lipolysis in human adipocytes without altering glucose uptake and differently from antipsychotic and antidepressant drugs with adverse effects on body weight control

Treatment with several antipsychotic drugs exhibits a tendency to induce weight gain and diabetic complications. The proposed mechanisms by which the atypical antipsychotic drug olanzapine increases body weight include central dysregulations leading to hyperphagia and direct peripheral impairment of fat cell lipolysis. Several investigations have reproduced in vitro direct actions of antipsychotics on rodent adipocytes, cultured preadipocytes, or human adipose tissue-derived stem cells. However, to our knowledge, no such direct action has been described in human mature adipocytes. The aim of the present study was to compare in human adipocytes the putative direct alterations of lipolysis by antipsychotics (haloperidol, olanzapine, ziprazidone, risperidone), antidepressants (pargyline, phenelzine), or anxiolytics (opipramol). Lipolytic responses to the tested drugs, and to recognized lipolytic (e.g., isoprenaline) or antilipolytic agents (e.g., insulin) were determined, together with glucose transport and amine oxidase activities in abdominal subcutaneous adipocytes from individuals undergoing plastic surgery. None of the tested drugs were lipolytic. Surprisingly, only opipramol exhibited substantial antilipolytic properties in the micromolar to millimolar range. An opipramol antilipolytic effect was evident against isoprenaline-, forskolin-, or atrial natriuretic peptide-stimulated lipolysis. Opipramol did not impair insulin activation of glucose transport but inhibited monoamine oxidase (MAO) activity to the same extent as antidepressants recognized as MAO inhibitors (pargyline, harmine, or phenelzine), whereas antipsychotics were inefficient. Considering its unique properties, opipramol, which is not associated with weight gain in treated patients, is a good candidate for drug repurposing because it limits exaggerated lipolysis, prevents hydrogen peroxide release by amine oxidases in adipocytes, and is thereby of potential use to limit lipotoxicity and oxidative stress, two deleterious complications of diabetes and obesity

Історія радянської України в бібліографічних покажчиках англомовних праць другої половини ХХ століття

У статті проаналізовано бібліографічні покажчики англомовної слов’янознавчої та радянознавчої літератури, видрукувані в англомовних країнах протягом другої половини ХХ ст. Зроблено спробу визначити місце, яке у них займали праці з історії України, зокрема ті, що стосуватися пізньосталінського та хрущовського періодів.В статье анализируются библиографические указатели англоязычной славяноведческой и советологической литературы, опубликованные в англоязычных странах во второй половине ХХ века. Сделана попытка охарактеризовать положение, которое в них занимала история Советской Украины, особенно ее позднесталинский и хрущевский периоды.In the article, the bibliographic guides to the English-language publications in Slavic, East European and Soviet Studies that were published in the second half of the 20th century are analyzed. The special attention is given to history of Ukraine from the second half of the 1940s till the mid-1960s as a particular subject in those guides