The Synthesis of Novel Analogues of the 4-quinolones

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Publisher :
ISBN 13 :
Total Pages : 0 pages
Book Rating : 4.:/5 (141 download)

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Book Synopsis The Synthesis of Novel Analogues of the 4-quinolones by : Stephen M. Courtney

Download or read book The Synthesis of Novel Analogues of the 4-quinolones written by Stephen M. Courtney and published by . This book was released on 1990 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt:

The Quinolones

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Publisher : Elsevier
ISBN 13 : 0080525784
Total Pages : 540 pages
Book Rating : 4.0/5 (85 download)

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Book Synopsis The Quinolones by : Vincent T. Andriole

Download or read book The Quinolones written by Vincent T. Andriole and published by Elsevier. This book was released on 2000-10-09 with total page 540 pages. Available in PDF, EPUB and Kindle. Book excerpt: Quinolones constitute a large class of synthetic antimicrobial agents that are highly effective in the treatment of many types of infectious diseases, particularly those caused by bacteria. New quinolones are continually being developed as bacterial species develop resistance to existing quinolones. This book presents the most current information available in our continual struggle to conquer disease. Over time, bacteria become resistant to medicines that are used to combat them. Because of this, the medical world is always in search of new and improved ways to battle these disease-causing bacteria. Quinolones are at the forefront of this research. Edited by one of the world's foremost authorities on the subject, the third edition of this highly successful title will serve as a valuable tool for primary care physicians and researchers interested in a comprehensive, up-to-date reference on the chemistry, mechanisms of action, development of resistance, and clinical efficacy of both currently available and newer quinolone compounds under investigation. This is the eagerly anticipated fully revised edition of the standard reference in the field. - Eagerly anticipated updated edition of noted title covering synthetic microbial agents that are useful against infectious disease, particularly those caused by bacteria - Edited by one of the foremost experts in the field of quinolone research and infectious disease - History of quinolones, chemistry & mechanisms of action, pharmacology, safety aspects - Role of quinolones in treating various types of infections, including respiratory infections, gastrointestinal infections, urinary tract infections, prostatitis, STDs and bacterial meningitis as well as their use in immunocompromised patients

A Continuous Process Towards the Synthesis of Quinolones

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Publisher :
ISBN 13 :
Total Pages : 112 pages
Book Rating : 4.:/5 (914 download)

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Book Synopsis A Continuous Process Towards the Synthesis of Quinolones by : Stevara N. Clinton

Download or read book A Continuous Process Towards the Synthesis of Quinolones written by Stevara N. Clinton and published by . This book was released on 2015 with total page 112 pages. Available in PDF, EPUB and Kindle. Book excerpt: The development of quinolones is described from the first quinolone to the latest fluoroquinolones. Quinolones have generated considerable interest since their discovery because of their antibacterial capabilities. Analogs incorporating the 4-quinolone ring system comprise a largely expanding group of synthetic compounds. The development of antibacterial resistance has created the need for an efficient synthesis of quinolones that can be easily adapted toward the assembly of quinolone based antibacterial drugs. There are several reported approaches to the 4-quinolone ring system. Many of these methods use expensive starting materials, require the removal of high boiling solvents, or use high temperature conditions (>200°C) for the final cyclization. Our synthesis of 4-quinolones was achieved via continuous flow chemistry using inexpensive starting materials in easily removable solvents, and under mild conditions. Flow chemistry is the use of technology that allows a continuous flow of reagents to be introduced at various points along a process stream, enabling interaction under highly controlled conditions. By employing this technology we achieved a more rapidly scalable synthesis of 4-quinolones, offering safer reacting conditions and highly reproducible results.

Investigations Into the Synthesis and Antibacterial Activity of Isoquinoline Analogues of the Antibacterial 4-quinolones

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Publisher :
ISBN 13 :
Total Pages : 0 pages
Book Rating : 4.:/5 (141 download)

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Book Synopsis Investigations Into the Synthesis and Antibacterial Activity of Isoquinoline Analogues of the Antibacterial 4-quinolones by : Ali M. Qaisi

Download or read book Investigations Into the Synthesis and Antibacterial Activity of Isoquinoline Analogues of the Antibacterial 4-quinolones written by Ali M. Qaisi and published by . This book was released on 1988 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt:

An Introduction to Drug Synthesis

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Publisher : Oxford University Press, USA
ISBN 13 : 0198708432
Total Pages : 587 pages
Book Rating : 4.1/5 (987 download)

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Book Synopsis An Introduction to Drug Synthesis by : Graham L. Patrick

Download or read book An Introduction to Drug Synthesis written by Graham L. Patrick and published by Oxford University Press, USA. This book was released on 2015 with total page 587 pages. Available in PDF, EPUB and Kindle. Book excerpt: Introduction to Drug Synthesis explores the central role played by organic synthesis in the process of drug design and development - from the generation of novel drug structures to the improved efficiency of large scale synthesis.

Antimicrobial Resistance

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Publisher : Springer Science & Business Media
ISBN 13 : 1475792034
Total Pages : 247 pages
Book Rating : 4.4/5 (757 download)

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Book Synopsis Antimicrobial Resistance by : Donald L. Jungkind

Download or read book Antimicrobial Resistance written by Donald L. Jungkind and published by Springer Science & Business Media. This book was released on 2013-06-29 with total page 247 pages. Available in PDF, EPUB and Kindle. Book excerpt: Development and Implications of Antimicrobial Resistance One of the most ominous trends in the field of antimicrobial chemotherapy over the past decade has been the increasing pace of development of antimicrobial resistance among microbial pathogens. The hypothesis that man can discover a magic bullet to always cure a particular infection has proved false. Physicians are now seeing and treating patients for which there are few therapeutic alternatives, and in some cases, none at all. Until recently there was little concern that physicians might be losing the war in our ability to compete with the evolving resistance patterns of microbial pathogens. Now the general public is very aware of the threat to them if they become infected, thanks to cover story articles in major magazines such as Time, Newsweek, newspapers, and other news sources. Antimicrobial resistance is not a novel problem. Shortly after the widespread introduction of penicillin in the early 1940s, the first strains of penicillin-resistant staphylococci were described. Today it is an uncommon event for a clinical laboratory to isolate an S. aureus that is sensitive to penicillin. Other gram-positive strains of bacteria have become resistant, including the exquisitely sensitive Streptococcus pneumoniae. Sensitivity to vancomycin was once so uniform that it was used in routine clinical laboratories as a surrogate marker for whether an organism should be classified as a gram-positive. That criterion can no longer be relied upon because of emerging resistance among some species. Gram-negative bacteria, viruses, fungi, and parasites all have succeeded in developing resistance.

Manual of Antimicrobial Susceptibility Testing

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Publisher : ASM Press
ISBN 13 : 9781555813499
Total Pages : pages
Book Rating : 4.8/5 (134 download)

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Book Synopsis Manual of Antimicrobial Susceptibility Testing by : Stephen J. Cavalieri

Download or read book Manual of Antimicrobial Susceptibility Testing written by Stephen J. Cavalieri and published by ASM Press. This book was released on 2009 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:

Synthetic Studies Towards Biologically Important Natural Products

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Publisher :
ISBN 13 :
Total Pages : 386 pages
Book Rating : 4.:/5 (116 download)

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Book Synopsis Synthetic Studies Towards Biologically Important Natural Products by : Ronald John Mastrolia III

Download or read book Synthetic Studies Towards Biologically Important Natural Products written by Ronald John Mastrolia III and published by . This book was released on 2017 with total page 386 pages. Available in PDF, EPUB and Kindle. Book excerpt: Rasapalli Research group is involved in Natural Products (NPs) based medicinal chemistry, specifically in developing synthetic access to biologically important natural products. Along those themes, this thesis consists of two parts. Part 1 deals with our work towards the total synthesis of the novel plant-derived aryltetralin cyclolignan linoxepin and some structurally related congeners that the synthetic scheme allows ready access to. As an introduction, a brief review of lignan natural products especially Podophyllotoxin and its most clinically important derivatives is provided. These agents and others like them inhibit/poison the eukaryotic variants of topoisomerase II enzymes. They are thereby endowed with anti-tumor cell properties. The structure of linoxepin, our target, is of a similar aryltetralin lignan compound like these well-known medicines it is of immense synthetic organic as well as medical interest to develop reliable syntheses of novel lignan molecules such as this as they show potential for useful bioactivities by the successful precedents set by older members of their chemical class. Our group proposed a scheme that hinged on an intramolecular dehydro Diels-Alder (DDA) reaction that would be utilized to construct the entire aryltetralin core of linoxepin. Once this was accomplished, an oxa-Pictet Spengler reaction was envisioned to complete the synthesis by forming linoxepin's synthetically challenging oxymethylene bridge and therefore constructing the compound's seven membered ring. The second part of this thesis deals with the synthesis of the recently isolated tetracyclic 4-quinolone compound quinolactacide. This is a natural product obtained from the endophytic fungus Penicillium citrinum in the South China Sea. A synthetic scheme for quinolactacide was developed involving only four chemical steps that also enabled the synthesis of two additional natural products found in similar fungal strains, marinamide and methylmarinamide. Methylmarinamide in fact an intermediate in our synthesis of quinolactacide. A short discussion of quinolone anti-bacterial quinolones and fluoroquinolones is offered, along with a brief look into the potential for novel 2, 3- disubstituted quinolone compounds as interesting drug leads against atypical protazoal pathogens. Our scheme is shown to also allow for the production of a library of such compounds. It is hoped that quinolactacide could exhibit activity as it contains the required binding groups that are also present in the successful anti-bacterial drug class, the quinolones. These act by poisoning bacterial DNA gyrase and killing the bacterial cell from the induced DNA damage. Some novel 2-substituted quinolones accessible from the scheme could also be primed for biological activities against some protazoal infections such as malaria. Extended pentacyclic quinolactacide analogues could potentially have anti-cancer activity as well, being structurally similar to some very well-known anti cancer compounds like camptothecin and indenoquinolones. Our scheme consisted mainly of a Claisen-type condensation reaction between isatoic anhydride and ketonitrile to produce the 4-quinolone nucleus in one chemical step. A Pinner reaction is then employed to convert the resulting nitrile intermediate into a methyl ester, itself methylmarinamide, which then undergoes pyridine-induced cyclization to afford the target lactam, quinolactacide. Hydrolysis of the same nitrile affords the natural product marinamide as well. Part 2 will also explore the simple synthesis of quinolactacide, marinamide, and methylmarinamide derivatives by both substitutions at nitrogen and by variation of the eastern most aromatic ring of the tetracyclic structure.

Transition-Metal-Mediated Aromatic Ring Construction

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Publisher : John Wiley & Sons
ISBN 13 : 111862999X
Total Pages : 785 pages
Book Rating : 4.1/5 (186 download)

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Book Synopsis Transition-Metal-Mediated Aromatic Ring Construction by : Ken Tanaka

Download or read book Transition-Metal-Mediated Aromatic Ring Construction written by Ken Tanaka and published by John Wiley & Sons. This book was released on 2013-07-09 with total page 785 pages. Available in PDF, EPUB and Kindle. Book excerpt: State-of-the-science methods, synthetic routes, and strategies to construct aromatic rings The development of new reactions for the synthesis of aromatic compounds is a highly active research area in organic synthesis, providing new functional organic materials, functional reagents, and biologically active compounds. Recently, significant advances in transition-metal-mediated reactions have enabled the efficient and practical construction of new aromatic rings with useful properties and applications. This book draws together and reviews all the latest discoveries and methods in transition-metal-mediated reactions, offering readers promising new routes to design and construct complex aromatic compounds. Integrating metal catalysis with aromatic compound synthesis, Transition-Metal-Mediated Aromatic Ring Construction offers a practical guide to the methods, synthetic routes, and strategies for constructing aromatic compounds. The book's five parts examine: [2+2+2], [2+2+1], and related cycloaddition reactions [4+2], [3+2], and related cycloaddition reactions Electrocyclization reactions Coupling and addition reactions Other important transformations, including methathesis reactions and skeletal rearrangement reactions Edited by Ken Tanaka, an internationally recognized expert in the field of transition-metal catalysis, the book features authors who are leading pioneers and researchers in synthetic reactions. Their contributions reflect a thorough review and analysis of the literature as well as their own firsthand laboratory experience developing new aromatic compounds. All chapters end with a summary and outlook, setting forth new avenues of research and forecasting new discoveries. There are also references at the end of each chapter, guiding readers to important original research reports and reviews. In summary, Transition-Metal-Mediated Aromatic Ring Construction offers synthetic chemists a promising new avenue for the development of important new aromatic compounds with a broad range of applications.

Quinolone Antimicrobial Agents

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Publisher :
ISBN 13 :
Total Pages : 572 pages
Book Rating : 4.3/5 (91 download)

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Book Synopsis Quinolone Antimicrobial Agents by : David C. Hooper

Download or read book Quinolone Antimicrobial Agents written by David C. Hooper and published by . This book was released on 1993 with total page 572 pages. Available in PDF, EPUB and Kindle. Book excerpt: Quinolones remain the most important class of antimicrobial agents discovered in recent years – over 1000 have been synthesized and evaluated. Since the publication of the original edition, considerable strides have been made in the research on structure–activity relationships, mechanism of action, resistance, pharmacodynamics and drug interactions. This edition consolidates and substantially updates our current state of knowledge of quinolones, with thirteen new chapters having been added.

Antimicrobial Chemotherapy

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Publisher : OUP Oxford
ISBN 13 : 0191628654
Total Pages : 409 pages
Book Rating : 4.1/5 (916 download)

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Book Synopsis Antimicrobial Chemotherapy by : Roger Finch

Download or read book Antimicrobial Chemotherapy written by Roger Finch and published by OUP Oxford. This book was released on 2012-01-05 with total page 409 pages. Available in PDF, EPUB and Kindle. Book excerpt: Antimicrobial agents are essential for the treatment of life-threatening infections and for managing the burden of minor infections in the community. In addition, they play a key role in organ and bone marrow transplantation, cancer chemotherapy, artificial joint and heart valve surgery. Unlike other classes of medicines, they are vulnerable to resistance from mutations in target microorganisms, and their adverse effects may extend to other patients (increased risk of cross-infection). As a consequence, there is a constant requirement for new agents, as well as practices that ensure the continued effective prescribing of licensed agents. Public awareness and concerns about drug resistant organisms has led to widespread publicity and political action in the UK, Europe and worldwide. The control of drug resistance and the implementation of good prescribing practice are now legal requirements in the UK as a result of the UK Health Act (2008). These fundamental changes underscore the need for a thorough understanding of the advantages and risks associated with specific antibiotic choices. This sixth edition of Antimicrobial Chemotherapy continues to be a valuable resource for undergraduates and graduates requiring a thorough grounding in the scientific basis and clinical application of these drugs. This new edition is updated to include the most recently licensed agents, notably in the treatment of viral infections including HIV/AIDS, and contains new guidance on prescribing practice and infection control practices that limit the development and spread of resistant organisms.

Bioactive Heterocycles

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Publisher : Nova Science Publishers
ISBN 13 : 9781622576364
Total Pages : 0 pages
Book Rating : 4.5/5 (763 download)

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Book Synopsis Bioactive Heterocycles by : K. L. Ameta

Download or read book Bioactive Heterocycles written by K. L. Ameta and published by Nova Science Publishers. This book was released on 2013 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is a critical and lucid account of various synthetic methodologies and biological activities of different sized bioactive heterocyclic compounds. In effect, this book imparts a great deal of comprehensive reviews about the chemistry and biology of selected groups of heterocycles and natural products including important pharmaceuticals as well as agrochemical pesticides in one handy project. Besides, this compendious effort encompasses different methods of synthesis and biological evaluation of heterocyclic compounds. The main purpose of this book is to share the recent advances and scope of Bioactive Heterocycles for the future avenues in the field. It has specifically been designed by keeping in mind the wide interests of individuals engaged in the design and synthesis of biologically active heterocyclic compounds as well as research scientists in academia and industry. The authors expect this book to be a standard reference in Universities and industrial libraries.

Quinolone Antibacterials

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Publisher : Springer
ISBN 13 : 9783642803666
Total Pages : 0 pages
Book Rating : 4.8/5 (36 download)

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Book Synopsis Quinolone Antibacterials by : Jochen Kuhlmann

Download or read book Quinolone Antibacterials written by Jochen Kuhlmann and published by Springer. This book was released on 2012-02-12 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: It has been over 30 years since the first clinically important member of the quinolone class, nalidixic acid, was introduced into medical practice. The modification produced in the quinolone nucleus by introducing a fluorine at the 6-position led to the discovery of the newer fluoroquinolones with enhanced antibacterial activities as compared to nalidixic acid. By now a great deal of preclinical and clinical experience has been obtained with these agents. The intense interest in this class of antibacterial agents by chemists, micro biologists, toxicologists, pharmacologists, clinical pharmacologists, and clini cians in various disciplines encouraged us to summarize the information on the history, chemistry, mode of action and in vitro properties, kinetics and efficacy in animals, mechanisms of resistance, toxicity, clinical pharmacology, clinical experience, and future prospects in one volume of the Handbook of Experimental Pharmacology. As this series deals predominantly with "experimental" characteristics of drugs, our volume is dedicated specifically to quinolones and emphasizes principally their preclinical and clinical phar macological characteristics, despite the existence of several summaries on quinolones. The chemistry of the quinolones is described in detail. The chapter on the mode of action of quinolones reports the conclusive evidence that gyrase is the intracellular target of the quinolones; however, another enzyme, topoisomerase IV, may also be a target for quinolones, and the exact mechanisms by which quinolones act bactericidally are far from being understood.

Nanostructures for Antimicrobial Therapy

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Publisher : Elsevier
ISBN 13 : 0323461514
Total Pages : 724 pages
Book Rating : 4.3/5 (234 download)

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Book Synopsis Nanostructures for Antimicrobial Therapy by : Anton Ficai

Download or read book Nanostructures for Antimicrobial Therapy written by Anton Ficai and published by Elsevier. This book was released on 2017-05-29 with total page 724 pages. Available in PDF, EPUB and Kindle. Book excerpt: Nanostructures for Antimicrobial Therapy discusses the pros and cons of the use of nanostructured materials in the prevention and eradication of infections, highlighting the efficient microbicidal effect of nanoparticles against antibiotic-resistant pathogens and biofilms. Conventional antibiotics are becoming ineffective towards microorganisms due to their widespread and often inappropriate use. As a result, the development of antibiotic resistance in microorganisms is increasingly being reported. New approaches are needed to confront the rising issues related to infectious diseases. The merging of biomaterials, such as chitosan, carrageenan, gelatin, poly (lactic-co-glycolic acid) with nanotechnology provides a promising platform for antimicrobial therapy as it provides a controlled way to target cells and induce the desired response without the adverse effects common to many traditional treatments. Nanoparticles represent one of the most promising therapeutic treatments to the problem caused by infectious micro-organisms resistant to traditional therapies. This volume discusses this promise in detail, and also discusses what challenges the greater use of nanoparticles might pose to medical professionals. The unique physiochemical properties of nanoparticles, combined with their growth inhibitory capacity against microbes has led to the upsurge in the research on nanoparticles as antimicrobials. The importance of bactericidal nanobiomaterials study will likely increase as development of resistant strains of bacteria against most potent antibiotics continues. - Shows how nanoantibiotics can be used to more effectively treat disease - Discusses the advantages and issues of a variety of different nanoantibiotics, enabling medics to select which best meets their needs - Provides a cogent summary of recent developments in this field, allowing readers to quickly familiarize themselves with this topic area

Comprehensive Organic Chemistry Experiments for the Laboratory Classroom

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Publisher : Royal Society of Chemistry
ISBN 13 : 1849739633
Total Pages : 976 pages
Book Rating : 4.8/5 (497 download)

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Book Synopsis Comprehensive Organic Chemistry Experiments for the Laboratory Classroom by : Carlos A. M. Afonso

Download or read book Comprehensive Organic Chemistry Experiments for the Laboratory Classroom written by Carlos A. M. Afonso and published by Royal Society of Chemistry. This book was released on 2016-12-16 with total page 976 pages. Available in PDF, EPUB and Kindle. Book excerpt: This expansive and practical textbook contains organic chemistry experiments for teaching in the laboratory at the undergraduate level covering a range of functional group transformations and key organic reactions.The editorial team have collected contributions from around the world and standardized them for publication. Each experiment will explore a modern chemistry scenario, such as: sustainable chemistry; application in the pharmaceutical industry; catalysis and material sciences, to name a few. All the experiments will be complemented with a set of questions to challenge the students and a section for the instructors, concerning the results obtained and advice on getting the best outcome from the experiment. A section covering practical aspects with tips and advice for the instructors, together with the results obtained in the laboratory by students, has been compiled for each experiment. Targeted at professors and lecturers in chemistry, this useful text will provide up to date experiments putting the science into context for the students.

DNA Topology

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Publisher : Oxford University Press, USA
ISBN 13 : 9780198567097
Total Pages : 224 pages
Book Rating : 4.5/5 (67 download)

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Book Synopsis DNA Topology by : Andrew D. Bates

Download or read book DNA Topology written by Andrew D. Bates and published by Oxford University Press, USA. This book was released on 2005 with total page 224 pages. Available in PDF, EPUB and Kindle. Book excerpt: "A key aspect of DNA is its ability to form a variety of structures, this book explains the origins and importance of such structures"--Provided by publisher.

Antibiotic Discovery and Development

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Publisher : Springer Science & Business Media
ISBN 13 : 1461414008
Total Pages : 1119 pages
Book Rating : 4.4/5 (614 download)

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Book Synopsis Antibiotic Discovery and Development by : Thomas J. Dougherty

Download or read book Antibiotic Discovery and Development written by Thomas J. Dougherty and published by Springer Science & Business Media. This book was released on 2011-12-18 with total page 1119 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.