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Dissertations / Theses on the topic 'Β-lactams'

Author: Grafiati

Published: 4 June 2021

Last updated: 26 July 2025

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1

Goh, Kee Chuan. "The biosynthesis of β-lactams". Thesis, University of Oxford, 1993. http://ora.ox.ac.uk/objects/uuid:24b6b29d-87cc-48f2-bd1b-bb64c663604f.

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This thesis reports the work done on two research projects which were carried out independently of each other but converge on the central theme of β-lactam biosynthesis. Chapter 1 provides an overview of biosynthesis in secondary metabolism, with special emphasis on current knowledge about the β-lactams. The first project, covered from Chapters 2 to 5, was part of our group's continuing effort to understand the structure and mechanism of Ring Expandase-Hydroxylase (REXH), an enzyme involved in the biosynthesis of cephalosporin C in Cephalosporium acremonium. REXH is a bifunctional enzyme, conv

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2

Joshi, S. N. "Diastereoselective synthesis of β-lactams". Thesis(Ph.D.), CSIR-National Chemical Laboratory, Pune, 2000. http://dspace.ncl.res.in:8080/xmlui/handle/20.500.12252/2271.

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3

Jayaraman, M. "Asymmetric synthesis of β-lactams". Thesis(Ph.D.), CSIR-National Chemical Laboratory, Pune, 1994. http://dspace.ncl.res.in:8080/xmlui/handle/20.500.12252/2803.

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4

Srirajan, V. "Diastereoselective synthesis of β - lactams". Thesis(Ph.D.), CSIR-National Chemical Laboratory, Pune, 1996. http://dspace.ncl.res.in:8080/xmlui/handle/20.500.12252/3378.

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5

Thiagarajan, K. "Studies in β-lactams synthesis". Thesis(Ph.D.), CSIR-National Chemical Laboratory, Pune, 2002. http://dspace.ncl.res.in:8080/xmlui/handle/20.500.12252/2853.

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6

Betou, Marie. "Semipinacol rearrangement of cis-fused β-lactam diols into bicyclic lactams". Thesis, University of Birmingham, 2013. http://etheses.bham.ac.uk//id/eprint/4348/.

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The 6-azabicyclo[3.2.1]octane ring system is found in a wide variety of biologically active natural and non-natural products. The aim of this project is to prepare the 7,8-diketo-6-azabicyclo[3.2.1]octane structure via a semipinacol rearrangement of ring-fused β -lactams. Chapter 1 introduces the pinacol and semipinacol rearrangement, including the use of cyclic sulfites and phosphoranes, and ring expansion of β -lactams. Previous work in the Grainger group for the synthesis of lactams via tandem radical cyclisation-dithiocarbamate group transfer is also discussed. Chapter 2 describes the meth

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7

Naz, Summia. "A calorimetric study of β-sultams and β-lactams". Thesis, University of Huddersfield, 2009. http://eprints.hud.ac.uk/id/eprint/6975/.

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The hydrolytic degradation of a series of β-sultams and β-lactams was investigated using isothermal microcalorimetry (IMC), to determine kinetic and enthalpic data. The importance of these studies was to model the process of hydrolysis as this was a simplification of the mechanism by which β-lactams and β-sultams function as serine protease inhibitors. Calorimetric studies were conducted using a Thermal Activity Monitor (TAM 2277). Three categories of experiments were conducted: in the solid state, varying relative humidity (R/H) and in aqueous solution. Hydrolytic rate constants and enthalpie

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8

Fontana, Francesco. "Stereoselective synthesis of β-lactams and carpanone derivatives". Paris 6, 2008. http://www.theses.fr/2008PA066441.

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SECTION A Nous décrivons la synthèse de nouveaux dérivés 4-spiro--lactamiques, au moyen de réactions de Staudinger entre des cétènes dérivant des -aminoacides cycliques énantiopurs (dérivés protégés de l’acide 1,3-thiazolidine-2-carboxylique et de la 4-hydroxy-L-proline) et des imines riches en électrons. Nous avons ensuite évalué la réactivité des composés obtenus conduisant à des produits -lactamiques mono- ou polycycliques totalement nouveaux et intéressants. SECTION B La carpanone est un lignane possédant cinq centres stéréogènes contigus qui a été isolée sous forme racémique de l'arbre

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9

Kale, A. S. "Studies in synthesis and transformations of β-lactams". Thesis(Ph.D.), CSIR-National Chemical Laboratory, Pune, 2007. http://dspace.ncl.res.in:8080/xmlui/handle/20.500.12252/2613.

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10

Chappell, Benjamin Graham Neil. "A general catalytic β-C-H carbonylation of aliphatic amines to β-lactams". Thesis, University of Cambridge, 2018. https://www.repository.cam.ac.uk/handle/1810/274756.

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Carbonyl compounds are of central importance to organic chemistry and their reactions have been described as the ‘backbone of organic synthesis’. Over recent decades, palladium-catalysed C–H carbonylation reactions have emerged as a powerful means of introducing carbonyl motifs to organic molecules. This thesis describes the development of a general C–H carbonylation reaction of secondary aliphatic amines, which provides facile access to synthetically useful β-lactam products. The first part of the thesis explores the scope and limitations of this reaction. Whilst previous C(sp3)–H carbonylati

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11

Lefebvre, Anne-Laure. "Etude de l’activité in vitro des β-lactamines sur Mycobacterium abscessus et recherche de leurs cibles". Thesis, Sorbonne Paris Cité, 2015. http://www.theses.fr/2015USPCB107.

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Mycobacterium abscessus est une mycobactérie responsable principalement d’infections pulmonaires, en particulier chez les patients atteints de mucoviscidose ou de dilatation des bronches. M. abscessus est naturellement résistante aux antituberculeux, laissant peu d’options thérapeutiques. Le traitement de référence associait classiquement un aminoside, un macrolide (clarithromycine) et une β-lactamine (céfoxitine ou imipénème), avec un taux de succès d’environ 50 %. Cependant, des souches résistantes à la clarithromycine sont fréquemment isolées, remettant en cause l’utilisation de cet antibio

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12

Jackson, Lynn. "Inhibition of elastase and trypsin by novel β-lactams". Thesis, University of Edinburgh, 2002. http://hdl.handle.net/1842/15094.

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Elastase is a serine protease that has been implicated in a number of inflammatory conditions including rheumatoid arthritis and cystic fibrosis. These conditions are thought to result from an increased amount of active elastase in the body, caused by insufficient inhibition by endogenous inhibitors. Elastase has the ability to degrade many tissue components and this excessive tissue damage causes the onset of a variety of conditions. This knowledge has led to an increased interest in the production of elastase inhibitors with the hope of developing an inhibitor, which can be of therapeutic us

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13

Bhattacharya, Biplob. "Synthesis and Anti-MRSA Activity of Hydrophilic C3-Acylated N-Thiolated β-Lactams and N-Acyl Ciprofloxacin-N-Thiolated β-Lactam Hybrids". Scholar Commons, 2012. http://scholarcommons.usf.edu/etd/4289.

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The Turos laboratory has been working with N-thiolated β-lactams for years trying to understand the mode of action and structural features it needs to have biological activity. Over the years new data has shown promising inhibitory activity against various microbes. In this dissertation, a review of the vast amount of work carried out on N-thiolated β-lactams in Turos laboratory has been done and their novelty, in terms of structure and mechanism has been discussed. A complete outline of our work in the discovery and ongoing development of these compounds, starting from our initial, unexpected

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14

Cirillo, Martina <1994&gt. "β-lactams from their structural features to their biological applications". Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2022. http://amsdottorato.unibo.it/10378/1/%CE%B2-lactams%20from%20their%20structural%20features%20to%20their%20biological%20applications.pdf.

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β-lactam compounds represent an important class of four-membered cyclic amides (azetidin-2-ones) thanks to their valuable and varied biological activities. The presence of a β-lactam ring in a series of bioactive molecules targeting different proteins, allows us to consider the azetidin-2-one a privileged structure. The constrained four-membered cyclic amide could easily undergo ring-opening reactions by nucleophilic residues in the active sites of enzymes and this is the mechanism suggested for antibacterial activity; moreover, the rigid core structure could favour and actually enhance direct

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15

Shinkre, B. A. "Stereoselective synthesis of α-hydroxy acid derivatives and β lactams". Thesis(Ph.D.), CSIR-National Chemical Laboratory, Pune, 2004. http://dspace.ncl.res.in:8080/xmlui/handle/20.500.12252/2901.

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16

Edoo, Zainab. "Mechanism of L,D-transpeptidase inhibition by β-lactams and diazabicyclooctanes". Electronic Thesis or Diss., Sorbonne université, 2019. https://accesdistant.sorbonne-universite.fr/login?url=https://theses-intra.sorbonne-universite.fr/2019SORUS565.pdf.

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La résistance aux antibiotiques est une menace mondiale qui conduit à un besoin urgent de développement de nouveaux antibiotiques. L'étude du mécanisme d'inhibition des cibles des antibiotiques est cruciale pour le développement de nouvelles molécules. Le caractère essentiel du peptidoglycane, le composant majeur de la paroi bactérienne, ainsi que soixante-dix ans d'utilisation des β-lactamines ont fait de la polymérisation du peptidoglycane une cible attractive et validée pour les antibiotiques. Les protéines de liaison à la pénicilline (PLP) ont longtemps été considérées comme les seules enz

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17

Yao, Xiangyu. "Molecular mechanisms of spermine on its synergistic effect with beta-lactams against Staphylococcus aureus." Digital Archive @ GSU, 2012. http://digitalarchive.gsu.edu/biology_diss/121.

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Spermine (Spm), a potent bactericidal polyamine, exerts a strong synergistic effect with β-lactams against methicillin-resistant Staphylococcus aureus (MRSA) in a pH-dependent manner. At high pH (>8) Spm is a potent nucleophile, and able to form Spm-β-lactam adduct. At physiological pH (or lower), Spm carries positive charges, and can bind to DNA through charge interactions. The potential of Spm interfering with cell wall was first investigated. A spontaneous mutant of MRSA Mu50 selected for Spm resistance conferred resistance to Spm/β-lactam synergy. This phenotype was due to the presence of

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18

Dad, Mohammad M. (Mohammad Mehdj). "Aminoketene. Cycloaddition of Ketenes and Imines to Yield β- or δ- Lactams". Thesis, University of North Texas, 1991. https://digital.library.unt.edu/ark:/67531/metadc332534/.

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The purpose of this investigation was to provide a systematic study of the cycloaddition pf (N-alkyl-N-phenylamino)- methoxy-and dichloroketenes to various imines and to investigate the stereochemistry of these cycloadditions.

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19

Long, Timothy E. "N-Thiolated β-Lactams: Chemistry and Biology of a Novel Class of Antimicrobial Agents for MRSA". Scholar Commons, 2003. https://scholarcommons.usf.edu/etd/1420.

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N-Methylthio beta-lactams represent a promising new family of antibacterial agents whose in vitro activity is confined largely to Staphylococcus species, including multidrug-resistant forms of S. aureus. Originally developed in the 1980's for use as synthetic intermediates, N-methylthio beta-lactams have recently been shown in these laboratories to possess intriguing biological properties which are addressed in Chapters I-IV. In terms of the antibacterial activities, the structural features and species specificities exhibited by these compounds are unlike those of any existing family of beta-l

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20

PICCIRILLI, ALESSANDRA. "Biochemical and molecular characterization of GES and NDM engineered variants: interactions with β-lactams and inhibitors". Doctoral thesis, Università degli Studi dell'Aquila, 2019. http://hdl.handle.net/11697/148003.

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Antibiotic resistance occurs when bacteria causing an infection survive after being exposed to a drug that, under normal conditions, would kill it or inhibit its growth. As a result, these surviving strains multiply and spread due to the lack of competition from other strains sensitive to the same drug. Carbapenems and 3rd generation cephalosporins resistant Enterobacteriaceae represent one of the most critical group against which there is an urgent need to develop new antibiotics. These bacteria are common pathogens causing severe infections such as bloodstream infections, pneumonia, complica

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21

Shim, Jeung-Yeop. "Studies on Antibacterial Activities of N-Thiolated β-Lactams and Their Polymeric Nanoparticles Against MRSA". Scholar Commons, 2003. https://scholarcommons.usf.edu/etd/1476.

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Methicillin-resistant Staphylococcus Aureus (MRSA) is now the most challenging bacterial pathogen affecting patients in hospitals and in care centers, and has brought on the need to develop new drugs for MRSA. This thesis centers on studies of N-thiolated β-lactams, a new family of potent antibacterial compounds that selectively inhibit the growth of methicillin-resistant Staphylococcus aureus (MRSA). Chapter 1 describes MRSA in more detail. Chapter 2 outlines experiments on the effect of a fatty ester group (CO2R) on the C4-phenyl ring of N-methylthio β-lactams, expecting that attachment of l

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22

Emtenäs, Hans. "Synthesis and biological evaluation of Bicyclic β-Lactams and 2-Pyridinones : Pilicides Targeting Pilus Biogenesis in Pathogenic Bacteria". Doctoral thesis, Umeå universitet, Kemiska institutionen, 2003. http://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-165.

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New methods have been developed for the synthesis of bicyclic β-lactams and 2-pyridinones by combining acyl Meldrum’s acids and Δ2-thiazolines. The 2-pyridinones were synthesised both in solution using conventional heating or microwave assisted heating as well as by solid supported chemistry. The compounds (pilicides) were designed to interfere with the assembly of pili in uropathogenic E. coli by inhibiting the periplasmic chaperones. The affinity of the pilicides to the chaperones was investigated with surface plasmon resonance technique (Biacore) and with relaxation-edited 1H NMR spectrosco

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23

Santos, Andressa Liberal. "Perfil fenotípico e genotípico de enterobactérias resistentes aos beta-lactâmicos." Universidade Federal de Goiás, 2018. http://repositorio.bc.ufg.br/tede/handle/tede/8780.

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Wiedemann, Elija Nathan [Verfasser], та Armin [Akademischer Betreuer] Ofial. "Aliphatic and aromatic amines : C-H bond functionalization and kinetics of their reactions with β-lactones, β-lactams, and carbocationic electrophiles / Elija Nathan Wiedemann ; Betreuer: Armin Ofial". München : Universitätsbibliothek der Ludwig-Maximilians-Universität, 2019. http://d-nb.info/1199816663/34.

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25

Moro, Giulia <1993&gt. "Exploiting the intrinsic electro-activity of β-Lactams antibiotics: an electrochemical strategy for Cefquinome detection in raw milk samples". Master's Degree Thesis, Università Ca' Foscari Venezia, 2018. http://hdl.handle.net/10579/12221.

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The detection of beta-lactams antibiotic residues in milk is a fundamental issue for diary companies, consumers and authorities. On-site and rapid analytical tools as sensors are required to assure milk safety and quality. The electroactive behavior of certain antibiotic can be exploited for their detection, as for cefquinome (CFQ) or nafcillin (NAF). In this project, molecularly imprinted polymers (MIPs) electropolymerized on MCWNT modified screen-printed graphite electrodes (MWCNTs-G-SPEs) is proposed for the electrochemical detection of CFQ in raw milk. The electropolymerization was perfo

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26

Heldreth, Bart Allan. "N-Thiolated β-Lactams: Chemistry, SAR and Intracellular Target of a Novel Class of Antimicrobial and Anticancer Agents". Scholar Commons, 2004. https://scholarcommons.usf.edu/etd/1074.

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N-Thiolated β-lactams (1) represent a promising new group of compounds with potent inhibition effects on bacteria, like Bacillus anthracis and methicillin resistant Staphylococcus aureus, and onco-systems, like breast cancer and leukemia. Originally developed as part of a synthetic pathway to bicyclic lactams, N-thiolated β-lactams have been shown in this laboratory to possess intriguing biological activities. The antibacterial activities of this new class of agents rely on novel structural features unlike those of any existing family of β-lactam drugs. The lactams seem to exert their effects

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27

Dabos, Maria Laura Belen. "Structural and functional insights into the substrate specificity of OXA-48-like carbapenemases." Thesis, Université Paris-Saclay (ComUE), 2018. http://www.theses.fr/2018SACLS402/document.

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Les b-lactamines, grâce à leur efficacité clinique, sont parmi les antibiotiques les plus prescrits pour traiter des infections bactériennes. Cependant, leur utilité est compromise par la prolifération des b-lactamases (BLs) avec des profils d’hydrolyse de substrats très larges. La résistance induite par les BLs compromet également les b-lactamines les plus puissantes (c-à-d les carbapénèmes). OXA-48, une carbapénèmase de classe D (CHDL), a été initialement identifiée dans une souche de K. pneumoniae de Turquie en 2001. OXA-48 hydrolysent fortement les pénicillines, faiblement les carbapénèmes

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28

Cordillot, Mathilde. "Les L,D‐transpeptidases, cibles des carbapénèmes chez Mycobacterium tuberculosis." Thesis, Paris 5, 2013. http://www.theses.fr/2013PA05T030.

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Mycobacterium tuberculosis est responsable de 8,7 millions de nouveaux cas de tuberculose et de 1,4 millions de décès en 2011. L’émergence de souches résistantes aux deux antituberculeux majeurs, isoniazide et rifampicine, (MDR) et aux antibiotiques de seconde ligne (XDR), ainsi que la difficulté d’éradiquer les formes « dormantes » du bacille nécessitent la recherche de nouveaux antibiotiques. Les β-lactamines n’ont jamais été utilisées en thérapeutique car M. tuberculosis produit une β-lactamase à large spectre, BlaC. Cependant, l’association d’une β-lactamine appartenant à la classe des car

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29

Santos, Adailton Pereira dos. "Perfil de rastreamento de resistência das Pseudomonas aeruginosa e acompanhamento da rotina educacional." Universidade Federal de Goiás, 2018. http://repositorio.bc.ufg.br/tede/handle/tede/8698.

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Obwana, Balusaba-Arum. "Synergistic activities of the selected antibiotics of fluoroquinolones, β-lactams, aminoglycosides, glycopeptides and streptogramins against gentamicin-resistant Enterococcus faecalis and Enterococcus faecium". Thesis, University of Edinburgh, 2005. http://hdl.handle.net/1842/25035.

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The aim of this study was to investigate synergistic activities of the combined antibiotics against the gentamicin resistant <i>Enterococcus faecalis and Enterococcus</i> <i>faecium</i> and to establish the existence of some genes involved in the resistance of enterococci against gentamicin and ciprofloxacin. The total of 81 clinical isolates were collected for the study and all were found to be resistant to gentamicin (MICs range 32->256mg/l). 50 isolates were found to be resistant to ciprofloxacin with MICs range 64->256mg/l. The synergistic activities of the antibiotics combinations were es

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31

Marques, Andrea Cristina de Figueiredo. "O medicamento veterinário em Portugal: do registo à comercialização." Bachelor's thesis, Universidade Técnica de Lisboa. Faculdade de Medicina Veterinária, 2008. http://hdl.handle.net/10400.5/949.

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Dissertação de Mestrado Integrado em Medicina Veterinária<br>Esta dissertação tem por objectivo analisar as diversas áreas do medicamento veterinário farmacológico desde o registo, ou autorização de introdução no mercado (AIM), à sua comercialização. Após enquadramento legal, a abordagem de algumas áreas do medicamento veterinário farmacológico, nomeadamente no que se refere às propriedades farmacocinéticas e farmacodinâmicas e limite máximo de resíduos (LMR), foi ilustrada recorrendo a um medicamento concreto, o Rilexine 200 LC, como exemplo de caso. Porque a especialidade farmacêutica

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Hoyle, Anthony Michael. "The evolution β-lactam-β-lactamase inhibitor resistance in Escherichia coli". Thesis, University of Leeds, 2004. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.414282.

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Prosen, Katherine Rose. "Investigating the Mode of Action of a Novel N-sec-butylthiolated Beta-lactam Against Staphylococcus aureus." Scholar Commons, 2010. http://scholarcommons.usf.edu/etd/3609.

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N-sec -butylthioloated β-lactam (NsβL) is a novel beta-lactam antimicrobial with a mechanism of action proposed to inhibit 3-oxoacyl-acyl carrier protein synthase (ACP) III (FabH), resulting in the inhibition of fatty acid synthesis. It has been suggested that NsβL inhibits FabH indirectly by inactivating coenzyme-A (CoA). CoA is an essential cofactor for numerous proteins involved in glycolysis, the citric acid cycle (TCA), and pyruvate metabolism, in addition to fatty acid biosynthesis. This study aimed to determine the effects of NsβL on a diverse array of laboratory and clinical Staphyloc

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Franco, Andreia da Silva. "Infeção do trato urinário por Escherichia coli em cães e gatos : mecanismos moleculares de resistência aos antibióticos β-lactâmicos". Master's thesis, Universidade de Lisboa, Faculdade de Medicina Veterinária, 2017. http://hdl.handle.net/10400.5/13676.

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Dissertação de Mestrado Integrado em Medicina Veterinária<br>A infeção do trato urinário (ITU) é uma afeção frequentemente observada em clínica de animais de companhia, sendo uma das razões mais comuns para instituição de terapêutica antimicrobiana. Escherichia coli é o principal agente patogénico bacteriano associado a ITU. A resistência antimicrobiana de E. coli aos antibióticos β-lactâmicos representa um problema de saúde pública emergente uma vez que estes são frequentemente utilizados tanto em medicina veterinária como humana. O objetivo deste estudo foi caracterizar estirpes de E. coli i

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Kalu, Chimdi E., Noah Lyons, Abbas G. Shilabin та Chimdi Kalu. "Synthesis and Evaluation of 1,2,4-oxadiazolidinones: The Search for Potential non-β-lactam β-lactamase Inhibitors". Digital Commons @ East Tennessee State University, 2019. https://dc.etsu.edu/asrf/2019/schedule/159.

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β-lactam antibiotics have been the most widely used drug of choice to combat infectious disease caused by bacteria. Unfortunately, the effectiveness of these antibiotics is drastically threatened by bacterial β-lactamases. β-lactamases are currently responsible for the resistance to most β-lactam antibiotic drugs. For decades, β-lactam β-lactamases inhibitors have been used to reduce bacterial resistance, however, in this study, we will employ the use of 1,2,4-oxadiazolidinone derivatives as a non-β-lactam β-lactamases inhibitor against TEM-1 and P99 β-lactamases. The significance of oxadiazol

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Kalu, Chimdi Eke. "Synthesis and Evaluation of 1,2,4-oxadiazolidinones: The Search for A Potential Non-β-lactam β-lactamase Inhibitors". Digital Commons @ East Tennessee State University, 2019. https://dc.etsu.edu/etd/3578.

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β-lactam antibiotics have been the most widely used drug of choice to combat infectious disease caused by bacteria. Unfortunately, their effectiveness is drastically threatened by bacterial β-lactamases. β-lactamases is responsible for the resistance to most antibiotic drugs. For decades, β-lactam β-lactamases inhibitors have been used to reduce bacterial resistance; however, in this study 1,2,4-oxadiazolidinone derivatives as a non-β-lactam β-lactamases inhibitor against TEM-1 and P99 β-lactamases. The significance of oxadiazolidinone is the prominent five-membered ring scaffold in its struct

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Alorabi, Mohammed Abdullatif Abdullah. "Factors affecting metallo-β-lactamase production in the Enterobacteriaceae, and the impact on β-lactam resistance and fitness". Thesis, University of Bristol, 2017. https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.768192.

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38

Mathlouthi, Najla. "Déterminisme du support moléculaire et de l'épidémiologie de la résistance aux β-lactamines chez des bacilles à Gram négatif isolés dans des hôpitaux tunisiens et libyens". Thesis, Aix-Marseille, 2017. http://www.theses.fr/2017AIXM0079/document.

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L’augmentation et la dissémination de la résistance aux β-lactamines chez les bacilles à Gram négatif, particulièrement les Entérobactéries, les bactéries du genre Pseudomonas et Acinetobacter, représentent un problème majeur de santé publique. Les infections nosocomiales causées par ces bactéries multi-résistantes (BMR) ont conduit à une augmentation de la mortalité, de la morbidité et du coût de traitement. L’utilisation abusive et non contrôlée de ces antibiotiques a grandement contribué à la large diffusion de cette résistance. Ainsi, face à cette préoccupation mondiale et suite à de nombr

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39

Hussein, Marwa. "Development of new methodologies in organic synthesis for the preparation of bioactive molecules." Thesis, Rennes 1, 2017. http://www.theses.fr/2017REN1S046/document.

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La thèse est divisée en trois chapitres indépendants. Chimie du β-lactames : Synthèse d'α-éthylène et d'α-alkylidène-β-lactames en utilisant la réaction de Kinugasa. Chimie de l'acylsilane : application d'une réaction aldolique intramoléculaire asymétrique sur un dérivé d'acylsilane nouvellement synthétisé. - Chimie médicinale: synthèse de nouvelles molécules à but anticancéreux.Dans le premier chapitre la réaction de Kinugasa a été appliquée pour la première fois à des alcynes vrais, portant en position propargylique un groupe partant permettait d'accéder directement et en une étape aux méthy

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Arun, M. "Steroselective β-lactam ring construction". Thesis(Ph.D.), CSIR-National Chemical Laboratory, Pune, 2002. http://dspace.ncl.res.in:8080/xmlui/handle/20.500.12252/2856.

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41

Vali, Leila. "β-Lactam resistance in Haemophilus influenzae". Thesis, University of Edinburgh, 2005. http://hdl.handle.net/1842/25267.

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<I>Haemophilus influenzae</I> is the most important pathogen of <I>Haemophilus</I> genus in humans. Resistance to β-lactams has been documented in this species, however, most β-lactam antibiotics are still widely used for treatment of <I>H.influenzae</I> infections. In order to minimise treatment failure, the anti-microbial efficiency of drugs should be monitored regularly. In this study the prevalence of β-lacam resistance in clinical strains of <I>H.influenzae</I> was determined in Scotland. Six hundred and sixteen isolates were collected from four hospitals during 1993-1995. 20.5% of the st

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Jayanthi, A. "Studies in polycyclic β-lactam synthesis". Thesis(Ph.D.), CSIR-National Chemical Laboratory, Pune, 2005. http://dspace.ncl.res.in:8080/xmlui/handle/20.500.12252/2451.

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43

Keshri, Vivek. "Evolutionary analysis of the β-lactamase families". Thesis, Aix-Marseille, 2018. http://www.theses.fr/2018AIXM0250.

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Les antibiotiques β-lactamines sont parmi les médicaments antimicrobiens les plus anciens et les plus utilisés. L'enzyme bactérienne β-lactamase hydrolyse l'antibiotique β-lactame en cassant la structure de base "anneau β-lactame". Pour identifier les nouvelles β-lactamases, une étude complète a été réalisée dans diverses bases de données biologiques telles que Human Microbiome Project, env_nr et NCBI nr. L'analyse a révélé que les séquences ancestrales putatives et les recherches de profil HMM jouaient un rôle important dans l'identification de la base de données homologue et métagénomique à

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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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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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46

Gangwar, Sanjeev 1961. "Synthesis of β-lactamase inhibitors". Thesis, The University of Arizona, 1990. http://hdl.handle.net/10150/292028.

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Twenty-two compounds of the type R¹C₆H₄CH₂(CO)NHCHR²(CO)OCHR³COOH, where R¹ = H or OH, R² = H or Me, and R³ = H, Me, Et, i-Pr, Ph, or CH₂COOH, have been synthesized for testing as β-lactamase inhibitors. All of the intermediates and products were characterized by NMR, and mass spectra were run on some of the final products.

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Henlin, Jean-Michel. "Approches synthétiques d'antibiotiques potentiels de type β-lactame". Mulhouse, 1986. http://www.theses.fr/1986MULH0021.

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A partir de diazépine-1,2carboxylates-1 et de cétènes ou de chlorures d'acide, synthèse d'aza-3carbapérames et aza-3carbapénèmes-1 par l'intermédiaire d'azeto (1,2-b) diazépines-1,2 (a); additions de diels alder de a et de nitrosoformyl benzène : obtention d'oxo-4 benzamido-3 (dihydro oxazine-1,2yl-6)-2 azétidinecarbamates-1

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Khan, Tariq Hussain. "Approaches to the synthesis of β-lactam antibiotics". Thesis, University of Edinburgh, 1987. http://hdl.handle.net/1842/12361.

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Hayes, Michelle. "β-lactam and quinolone resistance in Aeromonas spp". Thesis, University of Edinburgh, 1995. http://hdl.handle.net/1842/20558.

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The majority of <I>Aeromonas</I> spp. are innately resistant to ampicillin, therefore the aim of this thesis was to examine the resistance mechanism of <I>A.salmonicida</I> subspp. <I>achromogenes</I> and <I>A.hydrophila</I> to β-lactam antibiotics. Previous researchers had revealed the presence of two β-lactamases in the motile <I>Aeromonas</I> spp., a penicillinase with carbapenemase activity and a cephalosporinase. However, it was demonstrated in this thesis, that these β-lactamases had not been purified completely and that three β-lactamases could be purified from <I>A.salmonicida</I> subs

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Madgwick, P. J. "Protein engineeing of β-lactamase I". Thesis, University of Oxford, 1986. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.375282.

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