Synthesis of β-Lactam Antibiotics PDF Download
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Author: Alle Bruggink
Publisher: Springer Science & Business Media
ISBN: 9401008507
Category : Science
Languages : en
Pages : 328
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Book Description
Penicillins and cephalosporins have a long history in combating bacterial infections. Despite new infectious diseases and occurring resistance, beta-lactam antibiotics will for many years to come continue to play a prominent role in our therapeutic arsenal. This book covers the industrial development of the chemical and biochemical processes used to manufacture these products, as well as looking ahead to possible future processes. The interplay between synthetic organic chemistry with the understanding and application of enzymes, modeling of fermentation processes and integration through (bio-) chemical process engineering is illustrated. In-depth scientific approaches to biocatalysis and biocatalyst development including enzyme kinetics, enzyme crystal studies and semi-rational enzyme mutations are also presented. Metabolic pathway analysis and modeling of fermentation process are treated as well as molecular precision in synthetic approaches to beta-lactams, their precursors and derivatives. Process technology studies including new reactor concepts, possible short-cut routes and improved down-stream-processing methods complete a broad view on the scope and limitations of the presently developed industrial processes including an intriguing insight into future process possibilities. This book represents an excellent case study on the transformation of traditional, stoïchiometric, organic synthesis and classical fermentations into modern (bio-) catalysis and biosynthesis based on insights in metabolic pathways and enzyme actions.
Author: Alle Bruggink
Publisher: Springer Science & Business Media
ISBN: 9401008507
Category : Science
Languages : en
Pages : 328
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Book Description
Penicillins and cephalosporins have a long history in combating bacterial infections. Despite new infectious diseases and occurring resistance, beta-lactam antibiotics will for many years to come continue to play a prominent role in our therapeutic arsenal. This book covers the industrial development of the chemical and biochemical processes used to manufacture these products, as well as looking ahead to possible future processes. The interplay between synthetic organic chemistry with the understanding and application of enzymes, modeling of fermentation processes and integration through (bio-) chemical process engineering is illustrated. In-depth scientific approaches to biocatalysis and biocatalyst development including enzyme kinetics, enzyme crystal studies and semi-rational enzyme mutations are also presented. Metabolic pathway analysis and modeling of fermentation process are treated as well as molecular precision in synthetic approaches to beta-lactams, their precursors and derivatives. Process technology studies including new reactor concepts, possible short-cut routes and improved down-stream-processing methods complete a broad view on the scope and limitations of the presently developed industrial processes including an intriguing insight into future process possibilities. This book represents an excellent case study on the transformation of traditional, stoïchiometric, organic synthesis and classical fermentations into modern (bio-) catalysis and biosynthesis based on insights in metabolic pathways and enzyme actions.
Author: Edwin H. Flynn
Publisher: Elsevier
ISBN: 1483270173
Category : Science
Languages : en
Pages : 769
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Book Description
Cephalosporins and Penicillins: Chemistry and Biology describes the studies made on cephalosporin in relation to the scientific and medicinal benefits that can be derived from cephalosporin C. This collection discusses how cephalosporin C is produced through modern isolation methods. One paper discusses its structure through chemical means, its degradation products, its derivative and other metabolic products such as penicillin N and cephalosporin P. Another paper explains the preparation method for 7-aminocephalosporanic acid and 6-aminopenicillanic acid through biological or chemical means. Another paper explains the alteration of the dihydrothiazine ring of the cephalosporins as the functionalities of these rings are chemically difficult to obtain. One paper also explains the rearrangements of cephalosporins and penicillins; cephalosporin can be synthesized from penicillin through an intermediacy of penicillin sulfoxide. Other papers discuss the pharmacology and toxicology of cephalosporins, as well as the practical tests and methods of assay that can be used in most cephalosporins, and in some cases, in penicillins. This book can prove useful for pharmacologists, microchemists, research workers, and technologists dealing with toxicology.
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: José-Luis Capelo-Martínez
Publisher: John Wiley & Sons
ISBN: 1119282527
Category : Medical
Languages : en
Pages : 730
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Book Description
This book presents a thorough and authoritative overview of the multifaceted field of antibiotic science – offering guidance to translate research into tools for prevention, diagnosis, and treatment of infectious diseases. Provides readers with knowledge about the broad field of drug resistance Offers guidance to translate research into tools for prevention, diagnosis, and treatment of infectious diseases Links strategies to analyze microbes to the development of new drugs, socioeconomic impacts to therapeutic strategies, and public policies to antibiotic-resistance-prevention strategies
Author: Hartmut Derendorf
Publisher: Lippincott Williams & Wilkins
ISBN: 1496385896
Category : Medical
Languages : en
Pages : 1334
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Book Description
Updated with the latest clinical advances, Rowland and Tozer’s Clinical Pharmacokinetics and Pharmacodynamics, Fifth Edition , explains the relationship between drug administration and drug response, taking a conceptual approach that emphasizes clinical application rather than science and mathematics. Bringing a real-life perspective to the topic, the book simplifies concepts and gives readers the knowledge they need to better evaluate drug applications.
Author: Thomas J. Dougherty
Publisher: Springer Science & Business Media
ISBN: 1461414008
Category : Medical
Languages : en
Pages : 1119
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Book Description
This volume covers all aspects of the antibiotic discovery and development process through Phase II/III. The contributors, a group of highly experienced individuals in both academics and industry, include chapters on the need for new antibiotic compounds, strategies for screening for new antibiotics, sources of novel synthetic and natural antibiotics, discovery phases of lead development and optimization, and candidate compound nominations into development. Beyond discovery , the handbook will cover all of the studies to prepare for IND submission: Phase I (safety and dose ranging), progression to Phase II (efficacy), and Phase III (capturing desired initial indications). This book walks the reader through all aspects of the process, which has never been done before in a single reference. With the rise of antibiotic resistance and the increasing view that a crisis may be looming in infectious diseases, there are strong signs of renewed emphasis in antibiotic research. The purpose of the handbook is to offer a detailed overview of all aspects of the problem posed by antibiotic discovery and development.
Author: Robert B. Morin
Publisher: Academic Press
ISBN: 1483277194
Category : Medical
Languages : en
Pages : 594
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Book Description
Chemistry and Biology of ?-Lactam Antibiotics, Volume 1: Penicillins and Cephalosporins provides information pertinent to the study of antibiotics containing the ?-lactam moiety. This book discusses the occurrence of a group of ?-lactam antibiotics structurally related to cephalosporin C. Organized into five chapters, this volume begins with an overview of the mechanism of action of ?-lactam antibiotics that caused many microbiologists to develop screening tools for the detection of the ?-lactam moiety. This text then discusses the discovery of the nocardicins, the thienamycins, and olivanic acids. Other chapters provide a summary of the essential penicillin sulfoxide chemistry that gave rise to many compounds. This book discusses as well the ability of chemists to predict the level of biological activity of a compound from knowledge of its structure through theoretical and physicochemical studies. The final chapter deals with quantitative structure–activity relationships. This book is a valuable resource for microbiologists, chemists, and scientists.
Author: Arnold L. Demain
Publisher: Springer
ISBN: 9783642819681
Category : Medical
Languages : en
Pages : 360
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Book Description
It is quite amazing that the oldest group of medically useful antibiotics, the p-Iactams, are still providing basic microbiologists, biochemists, and clinicians with surprises over 50 years after Fleming's discovery of penicillin production by Penicillium. By the end of the 1950s, the future of the penicillins seemed doubtful as resistant strains of Staphylococcus aureus began to increase in hospital populations. However, the development of semisynthetic penicillins provided new structures with resistance to penicillinase and with broad-spectrum activity. In the 1960s, the discovery of cephalosporin C production by Cephalosporium and its conversion to valuable broad-spectrum antibiotics by semisynthetic means excited the world of chemotherapy. In the early 1970s, the 40-year-old notion that p-lactams were produced only by fungi was destroyed by the discovery of cephamycin production by Streptomyces. Again this basic discovery was exploited by the development of the semisynthetic cefoxitin, which has even broader activity than earlier p-lactams. Later in the 1970 s came the discoveries of nocardicins from Nocardia, clavulanic acid from Streptomyces, and the carbapenems from Streptomyces. Now in the 1980s we learn that p-lactams are produced even by unicellular bacteria and that semisynthetic derivatives of these monobactams may find their way into medicine. Indeed, the future of the prolific p-lactam family seems brighter with each passing decade.
Author: Bimal Krishna Banik
Publisher: CRC Press
ISBN: 1040146619
Category : Science
Languages : en
Pages : 410
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Book Description
Due to their medicinal activity and potential use as synthetic starting materials, studies on beta-lactams have increased significantly. This unique volume takes readers on a tour de force from the concept of antibiosis to the serendipity of antibiotics, evolution of beta‐lactam development, and molecular biology of antibiotic resistance. These areas of research have culminated in a deeper understanding of microbiology, particularly in the area of bacterial cell wall synthesis and recycling. Considerable work has been performed by chemists and biologists to continue updating their findings about beta-lactam synthesis. Features: Stereoselective synthesis of monocyclic, bicyclic, and polycyclic beta-lactams Microwave, ultrasound, and solid support-mediated preparation of beta-lactams Diverse medicinal activities including anticancer activities of beta-lactams and products obtained from them Nanoparticles, artificial intelligence, and dipole moments in beta-lactam science Synthesis and mechanism of formation of polyaromatic beta-lactams
Author: Rosaleen Anderson
Publisher: John Wiley & Sons
ISBN: 1118325443
Category : Science
Languages : en
Pages : 379
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Book Description
Antibacterial agents act against bacterial infection either by killing the bacterium or by arresting its growth. They do this by targeting bacterial DNA and its associated processes, attacking bacterial metabolic processes including protein synthesis, or interfering with bacterial cell wall synthesis and function. Antibacterial Agents is an essential guide to this important class of chemotherapeutic drugs. Compounds are organised according to their target, which helps the reader understand the mechanism of action of these drugs and how resistance can arise. The book uses an integrated “lab-to-clinic” approach which covers drug discovery, source or synthesis, mode of action, mechanisms of resistance, clinical aspects (including links to current guidelines, significant drug interactions, cautions and contraindications), prodrugs and future improvements. Agents covered include: agents targeting DNA - quinolone, rifamycin, and nitroimidazole antibacterial agents agents targeting metabolic processes - sulfonamide antibacterial agents and trimethoprim agents targeting protein synthesis - aminoglycoside, macrolide and tetracycline antibiotics, chloramphenicol, and oxazolidinones agents targeting cell wall synthesis - β-Lactam and glycopeptide antibiotics, cycloserine, isonaizid, and daptomycin Antibacterial Agents will find a place on the bookshelves of students of pharmacy, pharmacology, pharmaceutical sciences, drug design/discovery, and medicinal chemistry, and as a bench reference for pharmacists and pharmaceutical researchers in academia and industry.
