Macrolide Antibiotics As Anti Bacterial And Potential Anti Malarial Medicines
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Macrolide Antibiotics As Anti Bacterial And Potential Anti Malarial Medicines
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Author : Biljana Arsic
language : en
Publisher:
Release Date : 2012
Macrolide Antibiotics As Anti Bacterial And Potential Anti Malarial Medicines written by Biljana Arsic and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012 with categories.
Macrolide antibiotics are known as anti-bacterial agents. Erythromycin A, 14-membered macrolide antibiotic is known to exist in two forms-ketone (active) and hemiacetal form (inactive). It shows mild flexibility in silico. Its derivative, clarithromycin, 6-O-methyl erythromycin A, shows rigidity and activity against Gram-positive bacteria. The semisynthetic derivative of erythromycin A, azithromycin, 15-membered macrolide antibiotic, shows flexibility in silico and activity against Gram-negative bacteria. The combination of molecular modelling (molecular mechanics and/or molecular dynamics) with TRNOESY NMR data give us the active conformation of flexible molecules. Constraining the strong intramolecular hydrogen bonds can be helpful in the determination of the active conformation of the drug. We have developed modelling strategy for the construction of new 14- and 15-membered macrolideantibiotics with desired activity. Tylosin A and tylosin B, 16-membered macrolide antibiotics, show rigidity in silico. However, tylosin A is very unstable in aqueous solutions, so precise determination of hydrogen and carbon chemical shifts is extremely difficult. Nobody else before us tried to publish the full assignments of this compound in D2O. Accurate determination of hydrogen and carbon chemical shifts is necessary in order to further explore the properties of this compound. Anti-bacterial activity investigation of tylosin A and its derivative, tylosin B, shows lower activity both against Gram-positives and Gram-negatives compared to clarithromycin and azithromycin. Superposition of two molecules of azithromycin with one molecule of tylosin A reveals that two molecules of azithromycin actually occupy the space of one tylosin A molecule, which can explain found anti-malarial activity of tylosin A (both azithromycin and tylosin A show similar contacts to bacterial ribosomes).Clinical trials show that azithromycin has an anti-malarial activity. In order to investigate the potential anti-malarial activity of macrolide antibiotics, we had to construct the exit tunnel of the apicoplast ribosome from Plasmodium falciparum. Because of the unavailability of the crystal structure of P. falciparum ribosome (it is impossible to separate mitochondria and apicoplast, and both of them contain ribosomes), we used different computational methods and softwares in order to construct it. We used both homology modelling and ab initio modelling server for the construction of L4 (apicoplast-encoded P. falciparum ribosomal protein) and L22 (nuclear genome-encoded P. falciparum ribosomal protein) and RNA_2D3D software to construct the 23S rRNA from apicoplast ribosome of Plasmodium falciparum. Using Pymol software and MOE we have constructed the exit tunnel of apicoplast ribosome from P. falciparum. The model shows that it can bind one azithromycin molecule. It is the first model of the exit tunnel of the apicoplast ribosome from Plasmodium falciparum. Further work can be extended to the docking of other molecules than azithromycin into the modelled exit tunnel of Plasmodium falciparum.
Macrolides
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Author : Biljana Arsic
language : en
Publisher: Walter de Gruyter GmbH & Co KG
Release Date : 2018-03-19
Macrolides written by Biljana Arsic and has been published by Walter de Gruyter GmbH & Co KG this book supported file pdf, txt, epub, kindle and other format this book has been release on 2018-03-19 with Science categories.
Macrolide antibiotics represent a class of natural macrocyclic products, one of the most clinically important antibiotics. Unfortunately, the production and development of new macrolide antibiotics are not represented enough in the pharmaceutical industry today. The intention of the book is therefore not only to be a teaching tool for students and experts, but also to draw the attention of the general public to this extremely useful, cheap and relatively unharmful effective anti-macrobials, and potential anti-malarials. The authors introduce the different classes of macrolides and their derivatives, principles of their biological activity, their structure and interactions with biological targets as well as synthetic methods to produce new macrolide antibiotics of similar or improved properties. Special emphasis was put on conjugates of macrolides with nucleobases or nucleosides with numerous applications; among them the most important remains the attempt to overcome bacterial resistance.
Macrolide Antibiotics
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Author : W. Schönfeld
language : en
Publisher: Birkhäuser
Release Date : 2012-12-06
Macrolide Antibiotics written by W. Schönfeld and has been published by Birkhäuser this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012-12-06 with Medical categories.
There are only very few chemical classes of antibiotics in medical use, and these have originated over a span of more than 60 years of research. Almost half a century ago, the first member of the macrolides, erythromycin, was introduced as a treatment option for bacterial infections. Erythromycin is a very complex fermentation product obtained from the soil bacterium Saccharopolyspora ery thraea (originally named Streptomyces erythreus). The success of erythromycin, based on its efficacy and tolerability, stimulated researchers throughout the world to undertake intense efforts to understand the biology and chemistry of macrolides and to use this experience to improve the properties of this compound class. The second generation of macrolides, based on chemical modifications of erythromy cin, is currently being in broad use, especially for treatment of respiratory tract infections. We presently foresee the introduction of a new generation of macro lides, i. e. the ketolides, which have the potential to overcome rising resistance problems. This monograph is intended to give the interested reader an overview on "macrolide experience", covering important areas from basic research to clinical use. Starting from a historic overview, the essential basic parameters - efficacy, pharmacokinetics, pharmacodynamics, and pharmacology - are highlighted in order to introduce the reader to the rationale for clinical use of macrolides. The following group of chapters cover the complex chemistry of the macro lactone structures, giving historic background, basic structure-activity relation ships of various derivatization strategies, and perspectives for future discovery of new semisynthetic macrolide antibiotics.
Cdc Yellow Book 2018 Health Information For International Travel
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Author : Centers for Disease Control and Prevention CDC
language : en
Publisher: Oxford University Press
Release Date : 2017-04-17
Cdc Yellow Book 2018 Health Information For International Travel written by Centers for Disease Control and Prevention CDC and has been published by Oxford University Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2017-04-17 with Medical categories.
THE ESSENTIAL WORK IN TRAVEL MEDICINE -- NOW COMPLETELY UPDATED FOR 2018 As unprecedented numbers of travelers cross international borders each day, the need for up-to-date, practical information about the health challenges posed by travel has never been greater. For both international travelers and the health professionals who care for them, the CDC Yellow Book 2018: Health Information for International Travel is the definitive guide to staying safe and healthy anywhere in the world. The fully revised and updated 2018 edition codifies the U.S. government's most current health guidelines and information for international travelers, including pretravel vaccine recommendations, destination-specific health advice, and easy-to-reference maps, tables, and charts. The 2018 Yellow Book also addresses the needs of specific types of travelers, with dedicated sections on: · Precautions for pregnant travelers, immunocompromised travelers, and travelers with disabilities · Special considerations for newly arrived adoptees, immigrants, and refugees · Practical tips for last-minute or resource-limited travelers · Advice for air crews, humanitarian workers, missionaries, and others who provide care and support overseas Authored by a team of the world's most esteemed travel medicine experts, the Yellow Book is an essential resource for travelers -- and the clinicians overseeing their care -- at home and abroad.
Antibacterial Drug Discovery To Combat Mdr
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Author : Iqbal Ahmad
language : en
Publisher: Springer Nature
Release Date : 2019-11-09
Antibacterial Drug Discovery To Combat Mdr written by Iqbal Ahmad and has been published by Springer Nature this book supported file pdf, txt, epub, kindle and other format this book has been release on 2019-11-09 with Medical categories.
This book compiles the latest information in the field of antibacterial discovery, especially with regard to the looming threat of multi-drug resistance. The respective chapters highlight the discovery of new antibacterial and anti-infective compounds derived from microbes, plants, and other natural sources. The potential applications of nanotechnology to the fields of antibacterial discovery and drug delivery are also discussed, and one section of the book is dedicated to the use of computational tools and metagenomics in antibiotic drug discovery. Techniques for efficient drug delivery are also covered. The book provides a comprehensive overview of the progress made in both antibacterial discovery and delivery, making it a valuable resource for academic researchers, as well as those working in the pharmaceutical industry.
Antibiotic Drug Resistance
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Author : José-Luis Capelo-Martínez
language : en
Publisher: John Wiley & Sons
Release Date : 2019-09-24
Antibiotic Drug Resistance written by José-Luis Capelo-Martínez and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2019-09-24 with Medical categories.
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
The Global Impact Of Respiratory Disease
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Author : Darcy D. Marciniuk
language : en
Publisher:
Release Date : 2017
The Global Impact Of Respiratory Disease written by Darcy D. Marciniuk and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2017 with categories.
Drug Induced Liver Injury
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Author :
language : en
Publisher: Academic Press
Release Date : 2019-07-13
Drug Induced Liver Injury written by and has been published by Academic Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2019-07-13 with Medical categories.
Drug-Induced Liver Injury, Volume 85, the newest volume in the Advances in Pharmacology series, presents a variety of chapters from the best authors in the field. Chapters in this new release include Cell death mechanisms in DILI, Mitochondria in DILI, Primary hepatocytes and their cultures for the testing of drug-induced liver injury, MetaHeps an alternate approach to identify IDILI, Autophagy and DILI, Biomarkers and DILI, Regeneration and DILI, Drug-induced liver injury in obesity and nonalcoholic fatty liver disease, Mechanisms of Idiosyncratic Drug-Induced Liver Injury, the Evaluation and Treatment of Acetaminophen Toxicity, and much more. Includes the authority and expertise of leading contributors in pharmacology Presents the latest release in the Advances in Pharmacology series
Antimicrobial Agents
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Author : Varaprasad Bobbarala
language : en
Publisher: BoD – Books on Demand
Release Date : 2012-09-12
Antimicrobial Agents written by Varaprasad Bobbarala and has been published by BoD – Books on Demand this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012-09-12 with Medical categories.
This book contains precisely referenced chapters, emphasizing antibacterial agents with clinical practicality and alternatives to synthetic antibacterial agents through detailed reviews of diseases and their control using alternative approaches. The book aims at explaining bacterial diseases and their control via synthetic drugs replaced by chemicals obtained from different natural resources which present a future direction in the pharmaceutical industry. The book attempts to present emerging low cost and environmentally friendly drugs that are free from side effects studied in the overlapping disciplines of medicinal chemistry, biochemistry, microbiology and pharmacology.
Synthesis Of Essential Drugs
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Author : Ruben Vardanyan
language : en
Publisher: Elsevier
Release Date : 2006-03-10
Synthesis Of Essential Drugs written by Ruben Vardanyan and has been published by Elsevier this book supported file pdf, txt, epub, kindle and other format this book has been release on 2006-03-10 with Medical categories.
Synthesis of Essential Drugs describes methods of synthesis, activity and implementation of diversity of all drug types and classes. With over 2300 references, mainly patent, for the methods of synthesis for over 700 drugs, along with the most widespread synonyms for these drugs, this book fills the gap that exists in the literature of drug synthesis. It provides the kind of information that will be of interest to those who work, or plan to begin work, in the areas of biologically active compounds and the synthesis of medicinal drugs. This book presents the synthesis of various groups of drugs in an order similar to that traditionally presented in a pharmacology curriculum. This was done with a very specific goal in mind – to harmonize the chemical aspects with the pharmacology curriculum in a manner useful to chemists. Practically every chapter begins with an accepted brief definition and description of a particular group of drugs, proposes their classification, and briefly explains the present model of their action. This is followed by a detailed discussion of methods for their synthesis. Of the thousands of drugs existing on the pharmaceutical market, the book mainly covers generic drugs that are included in the WHO’s Essential List of Drugs. For practically all of the 700+ drugs described in the book, references (around 2350) to the methods of their synthesis are given along with the most widespread synonyms. Synthesis of Essential Drugs is an excellent handbook for chemists, biochemists, medicinal chemists, pharmacists, pharmacologists, scientists, professionals, students, university libraries, researchers, medical doctors and students, and professionals working in medicinal chemistry. * Provides a brief description of methods of synthesis, activity and implementation of all drug types* Includes synonyms* Includes over 2300 references