42 research outputs found

    Wavelength dependent photoextrusion and tandem photo-extrusion reactions of ninhydrin bis-acetals for the synthesis of 8-ring lactones, benzocyclobutenes and orthoanhydrides

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    Ninhydrin bis-acetals give access to 8-ring lactones, benzocyclobutenes and spirocyclic orthoanhydrides through photoextrusion and tandem photoextrusion reactions. Syntheses of fimbricalyxlactone B, isoshihunine and numerous biologically-relevant heterocycles show the value of the methods, while TA-spectroscopy and TD-DFT studies provide mechanistic insights on their wavelength dependence

    Determination of angiotensin I-converting enzyme activity in equine blood: lack of agreement between methods of analysis

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    Angiotensin-I converting enzyme (ACE) is a key regulator of blood pressure, electrolytes and fluid homeostasis through conversion of angiotensin I into angiotensin II. Recently, a genetic polymorphism of the ACE gene, which accounts for 47% of the variation of ACE activity in blood, has been advocated as a biomarker of athletic aptitude. Different methods of analysis and determination of ACE activity in plasma have been used in human and equine research without a consensus of a "gold standard" method. Different methods have often been used interchangeably or cited as being comparable in the existing literature; however, the actual agreement between assays has not been investigated. Therefore, in this study, we evaluated the level of agreement between three different assays using equine plasma obtained from 29 horses. Two spectrophotometric assays using Furylacryloyl-phenylalanyl-glycyl-glycine as substrate and one fluorimetric assay utilizing o-aminobenzoic acid-FRK-(Dnp)P-OH were employed. The results revealed that the measurements from the different assays were not in agreement, indicating that the methods should not be used interchangeably for measurement of equine ACE activity. Rather, a single method of analysis should be adopted to achieve comparable results and critical appraisal of the literature is needed when attempting to compare results obtained from different assays

    Guinea pig models for translation of the developmental origins of health and disease hypothesis into the clinic

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    Over 30 years ago Professor David Barker first proposed the theory that events in early life could explain an individual\u27s risk of non-communicable disease in later life: the developmental origins of health and disease (DOHaD) hypothesis. During the 1990s the validity of the DOHaD hypothesis was extensively tested in a number of human populations and the mechanisms underpinning it characterised in a range of experimental animal models. Over the past decade, researchers have sought to use this mechanistic understanding of DOHaD to develop therapeutic interventions during pregnancy and early life to improve adult health. A variety of animal models have been used to develop and evaluate interventions, each with strengths and limitations. It is becoming apparent that effective translational research requires that the animal paradigm selected mirrors the tempo of human fetal growth and development as closely as possible so that the effect of a perinatal insult and/or therapeutic intervention can be fully assessed. The guinea pig is one such animal model that over the past two decades has demonstrated itself to be a very useful platform for these important reproductive studies. This review highlights similarities in the in utero development between humans and guinea pigs, the strengths and limitations of the guinea pig as an experimental model of DOHaD and the guinea pig\u27s potential to enhance clinical therapeutic innovation to improve human health. (Figure presented.)

    Flow photochemical routes to indoles and 8-membered lactones, and their application in target synthesis

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    This thesis describes studies of two novel photochemical reactions towards 8-ring lactones and indoles, and the application of these products in target synthesis. Building on work by Bütenschon et al. and within the Harrowven group, the substrate scope of the photolysis of ninhydrin bis-acetals has been studied and expanded to the formation of 8-membered lactones. Meanwhile, the 8-membered lactone produced has been advanced to form cryptoacetalide, a natural component of the traditional Chinese medicine dan-shen, and a series of macrocycles which mirror the core structure of the resorcylic acid lactone family of natural products. This family exhibits a variety of biological activities and has been the subject of many natural product total syntheses which are reviewed herein. Furthermore, an oxidative flow photocyclisation of a variety of N-arylenaminones to indoles and carbozolones is described. Optimisations in respect to both yield and productivity are discussed in the context of a precursor to the WHO essential medicine, Ondansetron. These studies led us to design and develop novel experimental set-ups to conduct flow photochemical reactions at low temperatures and on large scales. Discussion of these reactors and their effectiveness is provided herein

    Dataset in support of the Southampton doctoral thesis 'Flow Photochemical Routes to Indoles and 8-membered Lactones, and their Application in Target Synthesis'

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    This file includes NMR data for all compounds seen in the thesis experimental, collected using NMR machines in B29, University of Southampton (use ACDLabs to view). It also includes IR data, collected on IR machine in B30, University of Southampton (Use ACDLabs to view). Also included is HRMS data collected by the MS department, B30, University of Southampton.</span

    Kiri N. Utkin'ile

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    Raimbach, Abraham, 1776-1843, inglise vasegraveerijaUtkin, Nikolai, 1780-1863, vasegraveerijaKunstiküsimuse

    Poems on the abolition of the slave trade

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    Gravure d\u27inspiration antique représentant un esclave, un aigle mort à ses côtés et un homme (probablement l\u27allégorie d\u27un dieu) penché vers lu
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