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Author: Andrew Giltrap
Publisher: Springer
ISBN: 9811088063
Category : Science
Languages : en
Pages : 285
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Book Description
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.
Author: Andrew Giltrap
Publisher: Springer
ISBN: 9811088063
Category : Science
Languages : en
Pages : 285
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Book Description
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.
Author: Sasadhar Majhi
Publisher: World Scientific
ISBN: 9811268703
Category : Science
Languages : en
Pages : 469
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Book Description
Modern Sustainable Techniques in Total Synthesis of Bioactive Natural Products comprises five parts for green tools, such as ultrasonic waves, microwave heating, visible-light photochemistry, organic electrochemistry, and flow chemistry, along with 72 chapters for each bioactive molecule of natural origin. Each chapter explores the natural source, structure, systematic name, structural features, compound class, biological activity, conventional approaches for their chemical synthesis, and demerit(s) of conventional approaches (where applicable). Finally, critical features of total synthesis using modern sustainable techniques, including reaction types, synthetic strategy, and synthetic route utilizing modern sustainable tools for each bioactive natural product and secondary metabolites, are discussed brilliantly. The spectrum of application of total synthesis of bioactive natural products using modern sustainable techniques may promote the development of more eco-friendly synthetic processes so that the next generations can live on this planet with a minimum energy requirement for chemical reactions with the least pollution.
Author: Goutam Brahmachari
Publisher: Elsevier
ISBN: 0081028237
Category : Science
Languages : en
Pages : 350
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Book Description
Total Synthesis of Bioactive Natural Products provides step-by-step guidelines for effectively synthesizing the most promising bioactive agents from a broad range of natural products. Beginning with a concise background that outlines the benefits and challenges faced in effective synthesis, the book goes on to provide individual outlines for approximately 100 of the most promising bioactive agents. Taking a logical, user-friendly approach, the systematic name, compound class, structure, natural source, pharmaceutical potential and synthetic routes for each structure are detailed, with clear illustrations throughout, making this book an essential and practical guide for anyone working with both synthesis and natural products. Provides individual outlines for the total synthesis of approximately 100 bioactive natural molecules Outlines each step of the process in detail, with full experimental information supported by extensive schemes Includes retrosynthetic analyses, reaction sequences and stereochemically crucial steps for each molecule
Author: Buzhe Xu
Publisher:
ISBN:
Category : Peptide antibiotics
Languages : en
Pages : 231
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Book Description
This thesis describes the first total synthesis of naturally occurring lanthipeptide tikitericin, as well as its N-terminal truncated analogues. The thesis also explores the total chemical synthesis of the lipopeptide antibiotic daptomycin and analogues along with evaluation of their antibacterial activity. Tikitericin is a newly described lanthipeptide characterized by four intramolecular thioether linked (methyl)lanthionine bridges. It was isolated from the New Zealand extremophilic microorganism Thermogemmatispora strain T81, collected at Tikitere (Hell's Gate), Rotorua. However, the chemical and biological properties of tikitericin haven't been established due to the limited amount of natural product isolated. This thesis describes the first total synthesis of tikitericin via Fmoc-solid-phase peptide synthesis (SPPS). The key noncanonical (methyl)lanthionine residues were synthesized in solution phase via an improved synthetic route and subsequently assembled to construct the peptide backbone using Fmoc-SPPS. N-Terminal truncated analogues of tikitericin were also prepared in order to evaluate the contribution of each sequential ring of the polycyclic lanthipeptide to the antibacterial activity. Daptomycin is a cyclic lipodepsipeptide natural product, exhibiting potent antimicrobial activity against highly resistant Gram-positive pathogens such as methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococci (VRE), and several species of Streptococci. Previous chemoenzymatic synthesis, semi-synthesis, and combinatorial biosynthesis only produced a very limited number of daptomycin analogues, leaving much of the chemical space unexplored. A de novo solid-phase synthesis of daptomycin via Boc chemistry was achieved. The challenging ester bond formation between the nonproteinogenic amino acid kynurenine was achieved by esterification of a threonine residue with a protected tryptophan. Subsequent late-stage on-resin ozonolysis, inspired by the biomimetic pathway, afforded the kynurenine residue directly. Synthetic daptomycin possessed potent antimicrobial activity against S. aureus, while five other daptomycin analogues containing (2R,3R)-3-methylglutamic acid, (2S,4S)-4-methylglutamic acid or canonical glutamic acid at position twelve prepared using this new methodology were all inactive; clearly establishing that the (2S,3R)-3-methylglutamic acid plays a key role in the antimicrobial activity of daptomycin.
Author: Jie Jack Li
Publisher: Springer Science & Business Media
ISBN: 3642340652
Category : Science
Languages : en
Pages : 292
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Book Description
'Total Synthesis of Natural Products' is written and edited by some of today's leaders in organic chemistry. Eleven chapters cover a range of natural products, from steroids to alkaloids. Each chapter contains an introduction to the natural product in question, descriptions of its biological and pharmacological properties and outlines of total synthesis procedures already carried out. Particular emphasis is placed on novel methodologies developed by the respective authors and their research groups. This text is ideal for graduate and advanced undergraduate students, as well as organic chemists in academia and industry.
Author: John ApSimon
Publisher: John Wiley & Sons
ISBN: 0470129506
Category : Science
Languages : en
Pages : 618
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Book Description
Each volume reviews the total synthesis of a set of compounds looking at syntheses reported historically and at the practice current at the time of publication. From volume 1 focusing on carbohydrates, prostagladins, nucleic acids, antibiotics, naturally occurring oxygen ring compounds and pyrrole pigments, the series continues with coverage of aromatic steroids, monoterpenes, triterpenes, sesquiterpenes, cannabinoids, natural inophores, insect pheromones and alkaloids. Volumes revisit the total synthesis of key compounds such as carbohydrates, nucleic acids and pyrrole pigments several times during the series building a picture of the historic development of total synthesis techniques for these major groups. Chapters are edited by experts in their field to give a complete overview of the best in the field at the time.
Author: John ApSimon
Publisher: Wiley-Interscience
ISBN: 047012959X
Category : Science
Languages : en
Pages : 720
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Book Description
The Total Synthesis of Natural Products Volume Seven Edited by John ApSimon This volume contains a chapter updating monoterpene synthesis and reviews the newer areas of leukotrienes and macrocyclic lactones. 1988 (0 471-88076-0) 480 pp. The Total Synthesis of Natural Products Volume Six Edited by John ApSimon Volume Six considers the total synthesis of triterpenes, carbohydrates, aromatic steroids, pyrrole pigments, and genes. 1984 (0 471-09900-7) 304 pp. The Total Synthesis of Natural Products Volume Five Edited by John ApSimon This present volume considers the total syntheses of sesquiterpenes, reflecting, in part, the heightened research activity in this area. 1983 (0 471-09808-6) 560 pp. The Total Synthesis of Natural Products Volume Four Edited by John ApSimon The fourth volume in this successful series offers synthetic approaches to a wide variety of natural products, including the synthesis of cannabinoids, natural inophores, insect pheromones, monoterpenes, and prostaglandins. 1981 (0 471-05460-7) 624 pp. The Total Synthesis of Natural Products Volume Three Edited by John ApSimon 1977 (0 471-02392-2) 576 pp. The Total Synthesis of Natural Products Volume Two Edited by John ApSimon 1973 (0 471-03252-2) 768 pp. The Total Synthesis of Natural Products Volume One Edited by John ApSimon 1973 (0 471-03251-4) 624 pp.
Author: Pei-Qiang Huang
Publisher: John Wiley & Sons
ISBN: 1118940210
Category : Science
Languages : en
Pages : 512
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Book Description
Uniting the key organic topics of total synthesis and efficient synthetic methodologies, this book clearly overviews synthetic strategies and tactics applied in total synthesis, demonstrating how the total synthesis of natural products enables scientific and drug discovery. • Focuses on efficiency, a fundamental and important issue in natural products synthesis that makes natural product synthesis a powerful tool in biological and pharmaceutical science • Describes new methods like organocatalysis, multicomponent and cascade reactions, and biomimetic synthesis • Appeals to graduate students with two sections at the end of each chapter illustrating key reactions, strategies, tactics, and concepts; and good but unfinished total synthesis (synthesis of core structure) before the last section • Compiles examples of solid phase synthesis and continuing flow chemistry-based total synthesis which are very relevant and attractive to industry R&D professionals
Author: Goutam Brahmachari
Publisher: World Scientific
ISBN: 9814335371
Category : Science
Languages : en
Pages : 695
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Book Description
Bioactive natural products are a rich source of novel therapeutics. Thus, the search for bioactive molecules from nature continues to play an important role in fashioning new medicinal agents. This volume, which comprises sixteen chapters written by active researchers and leading experts in natural products chemistry, brings together an overview of current discoveries in this remarkable field. It also provides information on the industrial application of natural products for medicinal purposes. This book will serve as a valuable resource for researchers to predict promising leads for developing pharmaceuticals to treat various ailments and disease manifestations.
Author: Stephen Hanessian
Publisher: Pergamon
ISBN:
Category : Science
Languages : en
Pages : 326
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Book Description
