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Total Synthesis of Natural Products with Antimicrobial Activity
ISBN-13:
9789811088063
Veröffentl:
2018
Seiten:
268
Autor:
Andrew Giltrap
Serie:
Springer Theses
eBook Typ:
PDF
eBook Format:
EPUB
Kopierschutz:
1 - PDF Watermark
Sprache:
Englisch
Beschreibung:
This thesis focuses on the development of efficient and scalable total syntheses of natural products that can be used as preferred scaffolds for anti-infective drug discovery. It describes the total synthesis of two classes of antimicrobial non-ribosomal peptides (NRPs) - teixobactin and the skyllamycins - with subsequent biological evaluation. The first part describes the first total synthesis of teixobactin by means of a solid-phase peptide synthesis-macrolactamisation approach, yielding a synthetic natural product that can combat a number of clinically relevant Gram-positive bacterial pathogens. The second part describes the first total synthesis of skyllamycins A-C, a family of structurally complex cyclic NRPs, which inhibit the growth of the Pseudomonas aeruginosa biofilms that are responsible for significant mortality among cystic fibrosis patients.
Introduction.- Total Synthesis of Teixobactin.- Synthesis of Deshydroxy Skyllamycins A-C.- Total Synthesis of Skyllamycins A-C.- Experimental.
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