Sökning: "ring-fused 2-pyridone"

Visar resultat 1 - 5 av 7 avhandlingar innehållade orden ring-fused 2-pyridone.

  1. 1. Peptidomimetics based on ring-fused 2-pyridones : probing pilicide function in uropathogenic E. coli and identification of Aβ-peptide aggregation inhibitors

    Författare :Veronica Åberg; Fredrik Almqvist; Jan Kihlberg; Morten Grötli; Umeå universitet; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; 2-pyridone; peptidomimetic; antibacterial; pili; Escherichia coli; virulence; amyloid; Alzheimer’s.; Organic chemistry; Organisk kemi;

    Sammanfattning : This thesis describes the synthesis and biological evaluation of highly substituted, ring-fused 2-pyridones. The utility of the bicyclic 2-pyridones to gain fundamental insights into the disease processes of bacterial infections and Alzheimer’s disease has been investigated. LÄS MER

  2. 2. Development of 2-Pyridone-based central fragments : Affecting the aggregation of amyloid proteins

    Författare :Magnus Sellstedt; Fredrik Almqvist; Petri Pihko; Umeå universitet; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; 2-pyridone; central fragment alteration; multi-component reactions; directed diversity-oriented synthesis; peptidomimetics; amyloid; protein aggregation; pilicide; curlicide; Biorganic Chemistry; bioorganisk kemi;

    Sammanfattning : There are many applications of small organic compounds, e.g. as drugs or as tools to study biological systems. Once a compound with interesting biological activity has been found, medicinal chemists typically synthesize small libraries of compounds with systematic differences to the initial “hit” compound. LÄS MER

  3. 3. Synthesis and functionalization of ring-fused 2-pyridones : Targeting pili formation in E. coli

    Författare :Nils Pemberton; Fredrik Almqvist; Oliver Kappe; Umeå universitet; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; 2-pyridone; acylketene; antibacterial; biofilm inhibitor; Mannich; Micro-wave-assisted chemistry; peptidomimetic; virulence.; Organic synthesis; Organisk syntes;

    Sammanfattning : Bicyclic dihydrothiazolo fused 2-pyridones have been studied as a new class of antibacterial agents, termed pilicides, that target the formation of adhesive bacterial surface organelles (pili) in pathogenic bacteria. Synthetic methods to further functionalize the bicyclic 2-pyridone scaffold have been developed in order to increase water-solubility and thereby facilitate biological evalua-tions. LÄS MER

  4. 4. Synthesis of substituted Ring-Fused 2-Pyridones and applications in chemical biology

    Författare :Christoffer Bengtsson; Fredrik Almqvist; Paul Helquist; Umeå universitet; []
    Nyckelord :Synthesis; 2-pyridone; 2-thiazoline; cross coupling; pili; curli; antibacterial; organisk kemi; Organic Chemistry;

    Sammanfattning : Antibiotics have been extensively used to treat bacterial infections since Alexander Fleming’s discovery of penicillin 1928. Disease causing microbes that have become resistant to antibiotic drug therapy are an increasing public health problem. LÄS MER

  5. 5. New alternatives to combat Listeria monocytogenes and Chlamydia trachomatis : Design, synthesis, and evaluation of substituted ring-fused 2-pyridones as anti-virulent agents

    Författare :Martina Kulén; Fredrik Almqvist; Anna Linusson Jonsson; Fritiof Pontén; Morten B. Strøm; Umeå universitet; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; Antibiotic resistance; anti-virulence; Listeria monocytogenes; Chlamydia trachomatis; ring-fused 2-pyridone; organic synthesis; structure-based design; PrfA; drug design; structure-activity relationship;

    Sammanfattning : Antibiotic resistance has become a global health burden with the number of resistant bacteria continuously increasing. Antibiotic drugs act by being either bactericidal (killing bacteria) or bacteriostatic (inhibiting growth of bacteria). However, these modes of action increase the selective pressure on the bacteria. LÄS MER