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Dissertations / Theses on the topic 'Bioactive Synthesis'

Author: Grafiati

Published: 6 September 2023

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1

Zheng, Zehua. "Synthesis of bioactive natural products." Thesis, University of British Columbia, 2016. http://hdl.handle.net/2429/59815.

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Crude extracts of the rare macrofungus Serpula sp. collected from a wooded area in Sri Lanka showed antimicrobial activity. The novel fungal metabolite serpulanine (2.1) was isolated from the crude extract in very small amounts along with a number of additional secondary metabolites. In order to obtain sufficient quantities of serpulanine (2.1) for biological evaluation, a synthetic route was developed to the natural product and a small library of analogs that have been evaluated in a panel of bioassays. Serpulanine (2.1) inhibits the histone deacetylase I/II with a clear dose response curve.

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2

Nelson, A. "Synthesis of bioactive indolizidine alkaloids." Thesis, Queen's University Belfast, 2005. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.421009.

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3

Shan, Yulong. "Bioactive carbohydrates : isolation, synthesis and conjugation." Thesis, Bangor University, 2011. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.556079.

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In this thesis four projects related to bioactive carbohydrates are described. The first project is about the extraction of iminosugars from Hyacinthoides non-scripta. This is the first time that extraction from English bluebell seeds has been described. Efficient extraction and isolation methods are reported. Another project discusses the development of a total synthetic carbohydrate conjugate vaccine candidate against Streptococcus pneumoniae type 14 using Gold nanoparticles as carrier. The synthetic pathway of the introduction of a linker for conjugation, and the deprotection of the tetrasa

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4

Carbain, Benoît. "A convenient synthesis of bioactive cyclohexenephosphonates." Thesis, University of Sussex, 2010. http://sro.sussex.ac.uk/id/eprint/2367/.

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Influenza virus infection and the shikimic acid pathway are two of many examples of microbe-host interactions and microbial biosynthetic pathways that are interesting for investigation by means of small molecules. A particularly interesting structural motif common to both is the cyclohexenecarboxylic acid. In the former, this structural motif has been employed as a mimetic of the sialyl cation intermediate and forms the scaffold of the anti-influenza drug and neuraminidase inhibitor Oseltamivir (or TamifluTM). In the latter pathway, crucial modifications towards aromatic amino acids are carrie

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5

Usai, Igor. "Synthesis of novel bioactive doxycycline derivatives." kostenfrei, 2008. http://www.opus.ub.uni-erlangen.de/opus/volltexte/2008/1082/.

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6

Hu, Yaogang. "Design and Synthesis of Bioactive Peptidomimetics." Scholar Commons, 2015. https://scholarcommons.usf.edu/etd/5504.

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Protein-Protein Interactions (PPIs) play a very important role in biological functions and therefore the inhibition of specific Protein-Protein Interactions has a huge therapeutic value. The most successful small molecular PPIs inhibitors do not fit with the prevalent `Rule of Five' drug profile. To overcome the disadvantages of small molecular PPIs inhibitors, peptide based PPIs inhibitors were developed. Herein we describe the development of a new class of peptidomimetics AA-peptides. The AApeptides were designed based on chiral PNA backbone. Substitution of nucleobases yields AApeptides tha

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7

Tyrrell, Andrew J. "Approaches to the synthesis of bioactive pyrrolizidines." Thesis, University of Oxford, 2008. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.497131.

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8

Miranda, Vanessa. "Synthesis of new bioactive autoinducer-2 analogues." Doctoral thesis, Universidade Nova de Lisboa, Instituto de Tecnologia Química e Biológica António Xavier, 2019. http://hdl.handle.net/10362/94059.

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" Bacteria behaviours are regulated on a communitywide scale by producing, secreting, detecting and responding to extracellular small signaling molecules (autoinducers) that accumulate in the environment in proportion to cell density. This process is called quorum sensing (QS). (...)"<br>N/A

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9

Isoni, Valerio. "Asymmetric synthesis of bioactive alkaloids from Amaryllidaceae." Thesis, University of Southampton, 2013. https://eprints.soton.ac.uk/355712/.

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A new route towards the diasteroselective synthesis of (+)-maritidine, a bioactive alkaloid from Amaryllidaceae, has been proposed. In our approach, an intramolecular Heck reaction was used to form the quaternary stereocentre C10b driven by the stereochemical information at C4a of the precursor. Allylic oxidation of intermediate 3.25 followed by diasteroselective reduction, introduced the alcohol at C3 with the correct stereochemistry. An advanced intermediate (3.29) in the synthesis of (+)-maritidine was produced, and routes to complete the total synthesis were proposed. A series of polymer-s

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10

Soldati, Roberto <1986&gt. "Synthesis of new bioactive β-lactam compounds". Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2015. http://amsdottorato.unibo.it/6974/1/Soldati_Roberto_Tesi.pdf.

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New biologically active β-lactams were designed and synthesized, developing novel antibiotics and enzymatic inhibitors directed toward specific targets. Within a work directed to the synthesis of mimetics for RGD (Arg-Gly-Asp) sequence able to interact with αvβ3 and α5β1-type integrins, new activators were developed and their Structure-Activity Relationships (SAR) analysis deepened, enhancing their activity range towards the α4β1 isoform. Moreover, to synthesize novel compounds active both against bacterial infections and pulmonary conditions of cystic fibrosis patients, new β-lactam candidat

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11

Soldati, Roberto <1986&gt. "Synthesis of new bioactive β-lactam compounds". Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2015. http://amsdottorato.unibo.it/6974/.

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New biologically active β-lactams were designed and synthesized, developing novel antibiotics and enzymatic inhibitors directed toward specific targets. Within a work directed to the synthesis of mimetics for RGD (Arg-Gly-Asp) sequence able to interact with αvβ3 and α5β1-type integrins, new activators were developed and their Structure-Activity Relationships (SAR) analysis deepened, enhancing their activity range towards the α4β1 isoform. Moreover, to synthesize novel compounds active both against bacterial infections and pulmonary conditions of cystic fibrosis patients, new β-lactam candidat

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12

Stevens, Kiri. "Methodology for the synthesis of NP25302 and other bioactive natural products." Thesis, University of Oxford, 2011. http://ora.ox.ac.uk/objects/uuid:ae18879e-d75e-4280-ba55-1ae08e64034f.

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Total synthesis of the pyrrolizidine alkaloid NP25302: (+)-NP25302 is an unusual vinylogous urea containing pyrrolizidine alkaloid shown to exhibit cell adhesion inhibition. It was envisaged that this natural product could be accessed by a novel 5-endo-dig cyclisation to construct the pyrrolizidine core, and a Curtius rearrangement to install the vinylogous urea motif. This methodology was first tested on a model system, furnishing nor-NP25302 from L-proline in 12 steps and 9% overall yield. The total synthesis of (±)-NP25302 was completed in 9 steps and 26% overall yield from ethyl 2-nitropro

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13

Lear, Sam. "Total synthesis of bioactive peptides and whole proteins." Thesis, Durham University, 2016. http://etheses.dur.ac.uk/11946/.

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Total chemical synthesis is an essential tool for the validation of natural product structures and the discovery and elaboration of novel therapeutic scaffolds. Chapter 1 (Part I) surveys existing treatments for trypanosomatid neglected tropical diseases, and the synthesis of a novel class of antiparasitic cyclic depsipeptides is reported (Chapter 2) alongside a full NMR assignment and structure calculation using NMR-derived distance restraints. The synthetic peptides exhibit activity profiles in agreement with published results, and a series of ester-to-amide substitution analogues also synth

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14

Chlubnová, Ilona. "Chemo-enzymatic synthesis of bioactive furanosyl-containing glycoconjugates." Rennes 1, 2010. http://www.theses.fr/2010REN1S196.

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Hexofuranoses are absent from mammals, but are present in numerous microorganisms, often highly pathogenic. This makes them very attractive targets for the development of new antimicrobial drugs. As an alternative to organic synthesis, the use of enzymes has been increasingly appreciated in the synthesis of glycoconjugates. Here we report the use of alpha-l-Arabinofuranosidase Araf51 for the synthesis of furanosyl-containing glycoconjugates. This enzyme was really efficient in catalysing oligomerisations of l-arabinofuranoside and d-galactofuranoside up to the formation of pentasaccharides, as

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15

Eaton, Alexander Lee. "Isolation and Synthesis of Bioactive Compounds from Plants." Diss., Virginia Tech, 2015. http://hdl.handle.net/10919/64367.

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As a part of a continuing search for bioactive compounds with the International Cooperative Biodiversity Group (ICBG), and in collaboration with the Natural Products Discovery Institute of the Institute for Hepatitis and Virus Research (IHVR), twelve plant extracts were investigated for their antiproliferative activity against the A2780 cell line, three plant extracts were investigated for their antimalarial activity against Plasmodium falciparum, and three plant extracts were investigated for their anti-inflammatory activity (PPAR-y inhibition). Bioassay-guided fractionation of extracts led t

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16

Chyan, Ming-Kuan. "Synthesis and Study of Bioactive Compounds: I. Pyrethroids; II. Glutathione Derivatives." Thesis, University of North Texas, 1995. https://digital.library.unt.edu/ark:/67531/metadc278848/.

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Part I: In the first study of pyrethroids, twenty-one novel pyrethroid esters bearing strong electron-withdrawing groups (e.g., halomethylketo and nitro groups) in the double bond side chain of the cyclopropane acid moiety have been synthesized and evaluated for insect toxicity. Rather than the usually employed Wittig reaction for these syntheses, the novel pyrethroid acid moieties were prepared by amino acidcatalyzed Knoevenagel condensations under mild conditions. In the second study of pyrethroids, fourteen pyrethroid-like carbonates were synthesized by condensation of a variety of alcohol

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17

Lahore, S. "¿SYNTHETIC STUDIES TOWARDS BIOACTIVE FUNGAL METABOLITES¿." Doctoral thesis, Università degli Studi di Milano, 2014. http://hdl.handle.net/2434/229905.

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The problem of the development of new pesticides is very urgent, mainly because of the appearance of pest forms resistant to permitted pesticides and for the strict requirements in terms of their safety for people and the environment. Small molecules produced in biological contexts have been, and still are, a large reservoir of new biologically active substances, which can become scaffolds for the discovery of new agrochemicals. The aim of this PhD work was to synthesize naturally occurring potentially antifungal and herbicidal compounds and to test their biological activity. Efforts mainl

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18

Semak, Vladislav. "Synthesis of 1S-ethyl-4-substituted quinolizidines and other potentially bioactive compounds." Doctoral thesis, Universitat de Barcelona, 2012. http://hdl.handle.net/10803/97241.

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Esta Tesis Doctoral se presenta como Compendio de publicaciones. Los capítulos en los que se ha dividido la presente Tesis son los siguientes: Capítulo 1 – parte A: Enantioselective, Protecting Group-Free Synthesis of 1S-Ethyl-4-Substituted Quinolizidines Se ha descrito una síntesis enantioselectiva que no implica grupos protectores para acceder a la quinolizidina clave 6 a partir de la lactama bicíclica derivada de fenilglicinol 1. La adición de un reactivo organometálico a 6 ocurre de manera estereoselectiva para conducir a las quinolizidinas 1S-etil-4-sustituidas 4-epi-207I y 7-9. Sigu

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19

Saito, Yu. "Synthesis of bioactive compounds: Synthetic study of D-Lac-terminated peptidoglycan fragment structures." Thesis, KTH, Kemiteknik, 2021. http://urn.kb.se/resolve?urn=urn:nbn:se:kth:diva-300085.

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Peptidoglycan (PGN) är en bakteriecellväggskomponent och känd för att känna igen olika receptorer eller enzymer för att leda aktiveringsimmunsystemet. Den allmänna strukturen för PGN består av sockerkedjor inklusive N-acetylglutamin (GlcNAc), N-acetylmuraminsyra (MurNAc) och tvärbundna peptidkedjor. PGN-fragment med D-Lac-ändpeptider har hittats från vankomycinresistenta enterokocker men ett kemiskt syntetiserat PGN-fragment med en D-Lac-ändpeptid har inte undersökts i detalj. Således fokuserade vi på syntesen av PGN-fragmentstrukturer som inkluderar en D-Ala-D-Lac-rest vid den terminala delen

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20

Pereira, Alban R. "Marine natural products : synthesis and isolation of bioactive analogues." Thesis, University of British Columbia, 2007. http://hdl.handle.net/2429/7526.

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Tauramamide (2-12), a linear acylpentapeptide recently isolated from cultures of Brevibacillus laterosporus (PNG-276) collected in Papua New Guinea, was synthesized in 9 steps and 29% overall yield. Besides confirming the proposed structure, synthetic (2-12) allowed the antimicrobial assessment of this novel antibiotic. Additionally, a new analogue of the surfactin depsipeptides family named dealkylsurfactin (2-48), was prepared in 10 steps and 14% overall yield. The compound was employed as a biological tool in binding studies between the mitotic regulator isomerase Pinl and the microtubule-a

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21

Hunter, Darren F. A. "Synthesis of bioactive pyrrolidine and piperidinone derivatives from carbohydrates." Thesis, University of Oxford, 2001. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.418528.

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22

Weston, Matthew. "Towards the asymmetric total synthesis of bioactive Celastraceae sesquiterpenoids." Thesis, University of Sheffield, 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.274986.

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23

Gill, Iqbal Singh. "Enzymatic synthesis of short bioactive peptides in novel media." Thesis, University of Reading, 1993. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.335913.

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24

Zerla, D. S. "Synthesis of chiral bioactive molecules by Catalytic Asymmetric Reduction." Doctoral thesis, Università degli Studi di Milano, 2009. http://hdl.handle.net/2434/147565.

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Synthesis of chiral bioactive molecules by Catalytic Asymmetric Reduction 1) Carnosine is an endogenous dipeptide (β-alanyl-L-histidine) presents in the human muscles and nerve tissue which has a protective and detoxifying effect on the toxic metabolites. D-Carnosine is cited as an equivalent to L-carnosine, but due to its durability to hydrolysis by the carnosinases, seems to produce better therapeutic results than the L-form. To study the bioavailability and pharmacokinetic profile of D-carnosine, a deuterium labelled derivative is needed. The optically active D or L histidine for car

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25

Straniero, V. "DESIGN AND SYNTHESIS OF NOVEL BIOACTIVE PEPTIDES AND PEPTIDOMIMETICS." Doctoral thesis, Università degli Studi di Milano, 2013. http://hdl.handle.net/2434/217536.

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Nowadays there’s a growing interest in biologically active peptides for the development of new therapeutics; however in some cases, they could not directly use as drugs, due to their inherent limitations, such as rapid metabolism and low oral activity. As a result, peptides are modified into peptidomimetics with specific characteristics, in a rational design. The present PhD project is focused on the synthesis of several peptides and peptidomimetics, structurally different and presenting individual features, properties, targets and pharmaceutical applications. In particular, two are the resea

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26

Stucchi, M. "MULTICOMPONENT APPROACHES TO THE SYNTHESIS OF SMALL BIOACTIVE MOLECULES." Doctoral thesis, Università degli Studi di Milano, 2015. http://hdl.handle.net/2434/330951.

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In this PhD thesis, we exploited the potentialities of four different multicomponent reactions (MCRs), namely Ugi four-component reaction (U-4CR), N-split Ugi reaction (N-split U-4CR), van Leusen three-component reaction (vl-3CR) and Biginelli reaction (Bg-3CR), developing five different approaches to the synthesis of small bioactive molecules. In particular, we successfully applied the build/couple/pair strategy obtaining a small library of ketopiperazine-based minimalist peptidomimetics, by means of diastereoselective U-4CR/post-cyclization sequences, employing optically pure amino acid-de

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27

Secci, Francesco. "Strained carbocyclic systems in the synthesis of bioactive products : methodologies and total synthesis." Paris 11, 2006. http://www.theses.fr/2006PA112296.

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28

Tang, Shoubin. "Structural and Synthetic Studies of Bioactive Natural Products." Diss., Virginia Tech, 2005. http://hdl.handle.net/10919/26104.

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As part of an ongoing investigation for anticancer agents from natural resources, four plant extracts were determined to contain interesting bioactivity. These extracts were separated by chromatography to afford a number of bioactive compounds that were characterized by spectral analysis. Fractionation of the fruit extract of Cryptocarya crassifolia led to the isolation of two known flavonoids and two known cryptocaryalactones. Fractionation of the bark extract of the same plant also gave the same two cryptocaryalactones. All these compounds were weakly active in a cytotoxicity assay.

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29

Tran, Wendy. "Synthesis of Bioactive Natural Products & Derivatives as Novel Anti-infectives." Thesis, University of Sydney, 2020. https://hdl.handle.net/2123/23995.

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Throughout history natural products have served as a valuable resource for the treatment of various diseases. To this day, many of these ancient remedies and their derivatives are still in use. However, in recent years, antibiotic discovery has stagnated at a time where there has also been the alarming emergence of antibiotic resistance which threatens to undermine the effectiveness of existing therapies. As such, novel antimicrobial agents are urgently needed that possess unique mechanisms of action to those currently in use. A promising class of natural products that exhibit antimicrobial ac

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30

Trippier, Paul Charles. "Synthesis of highly substituted heterocycles : the oxazolomycins." Thesis, University of Oxford, 2006. http://ora.ox.ac.uk/objects/uuid:b758987c-7a0c-4c1b-982c-61b4d383680a.

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This thesis is concerned with studies towards the total synthesis of a class of natural products - the oxazolomycins. Attention was focused on the left-hand side triene fragment and right-hand side lactam heterocyclic system. This thesis describes the synthesis of a racemic terminal phenyl analogue of oxazolomycin A and C, possessing the left-hand side triene geometry as required. A novel truncated pyridine analogue is also described. The molecules represent a racemic total synthesis of analogues of phthoxazolin A and inthomycins B and C. The synthesis is based upon a crucial Stille cross-coup

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31

Khanizeman, Rabi'ah Nisha. "Studies towards the synthesis of bioactive natural products and development of new synthetic methods." Thesis, Paris 6, 2017. http://www.theses.fr/2017PA066644.

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Plus de la moitié des médicaments mis sur le marché entre 1981 et 2014 sont des produits naturels ou des dérivés. Ainsi, les structures des produits naturels sont une excellente source d'inspiration pour la découverte de nouveaux médicaments. L'introduction de cette thèse met en lumière le rôle important joué par les produits naturels en chimie médicinale. De plus, la préparation de produits naturels peut déboucher sur le développement de nouvelles méthodes de synthèse. Ainsi, au cours de cette thèse une approche synthétique de plusieurs produits naturels a été réalisée. Ces composés présenten

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32

Kilburn, John Paul. "Novel solid-phase synthesis strategies for the preparation of heterocycles and guanidines." Thesis, Open University, 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.247056.

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33

Li, Sifeng. "Hydrofunctionalization of alkenes and their applications in the synthesis of bioactive compounds." HKBU Institutional Repository, 2020. https://repository.hkbu.edu.hk/etd_oa/812.

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Heterocycles are privileged structural motifs found in many natural products and biologically active compounds. Given the prevalence of this structural unit, there has been considerable interest and challenge in developing methods for construction optically pure heterocycles in organic synthesis and pharmaceutical chemistry. The skeleton of hydronaphthalene and indole are pervasive structural motifs in the pharmaceutical drugs that exhibit various bioactivities. This dissertation is mainly focused on the development of transition-metal-catalyzed asymmetric functionalization of alkenes, includi

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34

Xynos, Ioannis D. "Bioactive glasses for the in vitro synthesis of bone tissue." Thesis, Imperial College London, 2001. http://hdl.handle.net/10044/1/11494.

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35

Yan, Luping. "Bioactive marine natural products : analogue synthesis, SAR, and target identification." Thesis, University of British Columbia, 2014. http://hdl.handle.net/2429/50069.

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3,6,7-trihydroxycoumarin C11 (2.14) was first isolated from the green alga Dasycladus vermicularis in 1983. C11 and 3,7,8-trihydroxycoumarin C21 (2.15), alongside their precursors C12 (2.18) and C22 (2.20), were synthesized for a target-based screen for anti-HCV drugs, where ideal hits eliminate fluorescence signals by inhibiting the proteolytic activity of HCV NS3pro/Pep4A against a synthetic peptide “BS-IQFS”. With C12 and C22 serving as negative controls, C11 and C21 inhibited the NS3pro/Pep4A activity in vitro. The IC₅₀’s of C11 and C21 were 3.07 μM and 2.10 μM, respectively. A bioassay-g

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36

Blanc, Antoine. "Synthesis on the solid phase of a bioactive tryptathionine octreotate." Thesis, University of British Columbia, 2017. http://hdl.handle.net/2429/61821.

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Forestieri, Roberto. "Isolation, structure elucidation, and total synthesis of bioactive natural products." Thesis, University of British Columbia, 2013. http://hdl.handle.net/2429/45668.

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38

Shabbir, Ghulam. "The synthesis and mechanism of formation of some bioactive heterocycles." Thesis, University of Hertfordshire, 2000. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.365934.

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39

Almaliti, Jehad S. "Natural Products-Inspired Synthesis and Biological Evaluation of Bioactive Agents." University of Toledo Health Science Campus / OhioLINK, 2013. http://rave.ohiolink.edu/etdc/view?acc_num=mco1384555204.

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40

Antonopoulou, Io. "Use of feruloyl esterases for chemoenzymatic synthesis of bioactive compounds." Licentiate thesis, Luleå tekniska universitet, Kemiteknik, 2017. http://urn.kb.se/resolve?urn=urn:nbn:se:ltu:diva-62836.

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Feruloyl esterases (FAEs, EC 3.1.1.73) represent a subclass of carboxylic acid esterases that under normal conditions catalyze the hydrolysis of the ester bond between hydroxycinnamic acids (ferulic acid, sinapic acid, caffeic acid, p-coumaric acid) and arabinose residues in plant cell walls. Based on their specificity towards monoferulates and diferulates, substitutions on the phenolic ring and on their amino acid sequence identity, they have been classified into four types (A-D). The use of FAEs as accessory enzymes for the degradation of lignocellulosic biomass and their synergism with othe

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41

AMABILI, PAOLO. "α-Hydrazido acids for the synthesis of bioactive amphiphilic compounds". Doctoral thesis, Università Politecnica delle Marche, 2017. http://hdl.handle.net/11566/245568.

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Con lo scopo di ottenere nuovi foldameri (oligomeri con un folding prevedibile), sono stati sintetizzati nuovi mimici di β-peptidi caratterizzati dalla formale sostituzione Cβ→Nβ(acile) modificando β-amminoacidi a base pirrolidin-2-onica, utilizzati precedentemente nei nostri laboratori per la preparazione di esameri. Sono stati quindi sintetizzati nuovi oligomeri di α-idrazidoacidi conformazionalmente costretti in un anello imidazolidinonico (AOPIC) che sono stati poi analizzati usando tecniche spettroscopiche (NMR e CD) e computazionali (MD). Lo studio computazionale, oltre a fornire la prov

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42

Tinarelli, Alessandro <1975&gt. "Novel Methodologies for the Synthesis of Scaffolds for Bioactive Molecules." Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2010. http://amsdottorato.unibo.it/2291/1/Tinarelli-Alessandro-tesi.pdf.

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Tinarelli, Alessandro <1975&gt. "Novel Methodologies for the Synthesis of Scaffolds for Bioactive Molecules." Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2010. http://amsdottorato.unibo.it/2291/.

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44

Zang, Qin. "Towards the total synthesis of peloruside A analogues." Laramie, Wyo. : University of Wyoming, 2008. http://proquest.umi.com/pqdweb?did=1663059931&sid=1&Fmt=2&clientId=18949&RQT=309&VName=PQD.

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45

Stout, Elizabeth Paige. "Discovery and synthesis of bioactive natural product probes from marine systems." Diss., Georgia Institute of Technology, 2010. http://hdl.handle.net/1853/37301.

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Flora and fauna from terrestrial and marine environments provide libraries of natural compounds for drug discovery. The last four decades have seen major advances in ocean exploration that have allowed chemists and biologists to explore previously inaccessible and rare marine organisms. The study of under-explored marine organisms can result in the discovery of structurally novel and unusual natural products with drug potential. Prior to 2005, no natural products had been reported from the Fijian red macroalgae Callophycus serratus or Neurymenia fraxinifolia. As a result of the work described

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46

Chen, Xiaoyun [Verfasser]. "The synthesis of bioactive sulfoximines and N-alkynylated sulfoximines / Xiaoyun Chen." Aachen : Hochschulbibliothek der Rheinisch-Westfälischen Technischen Hochschule Aachen, 2014. http://d-nb.info/1066984204/34.

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47

Derudas, Marco. "Design, synthesis and biological evaluation of novel bioactive nucleosides and nucleotides." Thesis, Cardiff University, 2009. http://orca.cf.ac.uk/55855/.

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At the present there are 36 approved antiviral drugs in the UK of which half are nucleoside analogues. However, the emergence of drug resistance and of new virus strains necessitates new drugs. In particular in this thesis, different nucleoside analogues were studied as potential antivirals. One of the major issues related to nucleoside analogues is the emergence of resistance due to a lack of bioactivation to the monophosphate form. To overcome this issue, the phosphoramidate ProTide technology can be applied. This strategy allows the delivery of the monophosphate form directly inside the cel

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48

Montgomery, Laura Jane. "Investigations of the biosynthesis and biomimetic synthesis of bioactive natural products." Thesis, University of Warwick, 2008. http://wrap.warwick.ac.uk/4420/.

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This thesis describes work towards the biomimetic synthesis and understanding the biosynthesis of two families of natural products: prodiginines and quartromicins. Prodiginines are a large family of red pigmented tripyrrole antibiotics. Although they have not been used clinically, the promising anti-cancer, immunosuppressive and antimalarial activity they display at non-toxic doses has generated renewed interest in their utilisation. The synthesis of an analogue of the proposed pyrrole-2-carboxyl-RedO intermediate in prodiginine biosynthesis has been achieved. The resulting NAC thioester and a

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Filipa, P. da Cruz Ana. "C-branched carbohydrate lactones : Versatile intermediatesin the synthesis of branched bioactive." Thesis, University of Oxford, 2009. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.509913.

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Fara, Mario Antonio. "Cell penetrating peptoid carriers : microwave assisted synthesis and bioactive molecules delivery." Thesis, University of Edinburgh, 2008. http://hdl.handle.net/1842/10889.

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Effective methods for the selective passage of therapeutic molecules or probes through biological barriers are essential for the study of <i>cellular functions. </i>Cell penetrating cationic peptoids, based on a lysine like unit, were efficiently synthesised a combination of solid phase synthesis strategies and microwave heating. A linear 7mer peptoid was thus prepared by direct solid phase synthesis and conjugated to both a peptide hormone (α- Melanocyte Stimulating Hormone, a 13mer peptide) and to peptide nucleic acids (9mer, 12mer and 15mer prepared using Dde/Mmt protected monomers) target

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