Recent Developments in the Total Synthesis of Macrolide Antibiotics PDF Download
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Author:
Publisher:
ISBN:
Category :
Languages : en
Pages : 56
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Book Description
Author:
Publisher:
ISBN:
Category :
Languages : en
Pages : 56
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Author: John Powell Daub
Publisher:
ISBN:
Category :
Languages : en
Pages : 440
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Author: Gabor Lukacs
Publisher: Springer Science & Business Media
ISBN: 3642756174
Category : Science
Languages : en
Pages : 808
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Book Description
The use of antibiotics in the treatment by antibacterial and antifungal chemo therapy, has become standard practice since the end of World War Two and has had an enormous impact on healthcare throughout the world. Compounds belonging to this class have also reached an important place in the medical treatment of human cancer. Although, the discovery of most of these agents came from more or less sophisticated screening programs of soil microrganisms, many of the important antibiotics used today in clinical practice are derived from the original biosynthetic products by the application of often novel and generally elaborated chemical synthetic methodologies. In fact the antibiotics have represented (and still represent) for a generation of organic chemists an endless source of molecular structures whose varied assemblage of carbon atom backbones and chemical functions was beyond any possibility of imagination. Perhaps a similar repertoire of chemotypes was formerly offered by the natural products, namely the alkaloids, the terpenes, the vitamins and hormones as well as the pigments of the animal and plant kingdoms, albeit the chemical arrange ments of the antibiotic molecules appeared much more surprising and diverse to the admiring eyes of cultivated organic chemists. The idea of this book, certainly a landmark in the field, came during the Symposium of EUCHEM on Chemical Synthesis of Antibiotics, that was held at Aussois in Savoy, France (May 2-6, 1988), the initiative being taken by Gabor Lukacs to whom Masaji Ohno readily associated as a co-editor.
Author: Charles Tweedt Buse
Publisher:
ISBN:
Category : Antibiotics
Languages : en
Pages : 320
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Author: Xiao Jin
Publisher:
ISBN:
Category :
Languages : en
Pages : 227
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My Ph.D. research consists of two components: discovery of novel macrolide antibiotics and methodology development of N-sulfinyl metallodienamines. To tackle bacterial resistance, new antibiotics are desperately needed. My research objective is to address this need by designing, synthesizing, and evaluating novel macrolide antibiotics based on the best-in-class drug candidate, solithromycin. The drug discovery including following three projects: 1) Synthesis of solithromycin analogs wherein the desosamine sugar has been replaced with an acyclic amino alcohol surrogate; 2) In cellulo Click chemistry wherein the bacterial cell serves as the reaction vessel and the ribosome catalyzes the formation of triazole cycloadducts by testing different combinations of azide and alkyne fragments. One of the mechanisms of resistance to macrolide antibiotics is exemplified by methylation of A2058 by the methyltransferase encoded in erm genes. Methylation or dimethylation of A2058 leads to a steric clash with the macrolides and reduces the affinity of the macrolide for the ribosome. Thus, the bacterial resistant can be relieved via disrupting steric clashes between desosamine and A2058 residues. In 2017, I started a new project looking at the scope of the acyclic domino Michael/Mannich reaction to prepare chiral cyclohexenes developed by a previous group member, Dr. Vijay Chatare. This reaction is highly regioselective and stereoselective. Recent research showed that this reaction could be utilized on acroleins, acrylates and unsaturated ketones. Thus, we applied this useful methodology towards the concise total synthesis of (+)-ibogamine.
Author: Gabor Lukacs
Publisher:
ISBN:
Category : Medical
Languages : en
Pages : 990
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Author: Satoshi Omura
Publisher: Elsevier
ISBN: 0080535682
Category : Science
Languages : en
Pages : 655
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Book Description
Macrolide Antibiotics: Chemistry, Biochemistry, and Practice, Second Edition explores the discovery of new macrolide antibiotics, their function, and their clinical use in diseases such as cancer, AIDS, cystic fibrosis and pneumonia. This book discusses the creation of synthetic macrolides and the mechanisms of antibiotic activity. The uses for antimicrobial macrolides in clinical practice are also covered. This book is designed to appeal to both the basic and applied research communities interested in microbiology, bacteriology, and antibiotic/antifungal research and treament.
Author: I. J. Burnside
Publisher:
ISBN:
Category :
Languages : en
Pages :
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Author: Ian Stansfield
Publisher:
ISBN:
Category :
Languages : en
Pages :
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Author: Libing Yu
Publisher:
ISBN:
Category : Allene
Languages : en
Pages : 215
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From the microbial world, antibiotics are structurally complex and highly potent chemical weapons that co-evolved with bacteria. Macrolide (glycosylated cyclic polyketides) antibiotics have been used extensively as first-line antibacterial agents since the discovery of the broad-spectrum antibiotic erythromycin A in 1952. However wide-spread use of antibiotics has led pathogens to develop drug resistance. Therefore new and enhanced antibiotics are constantly in need. Described in this dissertation is my effort to emulate the synthetic capabilities of erythromycin-producing bacteria by accessing novel erythromycin-inspired polyketides via divergent total synthesis. New allene oxidation methods have been developed and implemented in a modular and divergent route to produce a diversified portfolio of cyclic polyketides and their glycoconjugates. I will disclose a total synthesis of 4,10-didesmethyl-(9S)-dihydroerythronolide A (Chapter 2), preparation of glycosylated erythromycin analogs (Chapter 3) and progress towards synthesis of 9(S)-dihydroerythronolide A (Chapter 4).
