Design, Synthesis, and Evaluation of Inhibitors of Trypanosome Growth for Neglected Disease Drug Discovery

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Publisher :
ISBN 13 :
Total Pages : 346 pages
Book Rating : 4.:/5 (915 download)

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Book Synopsis Design, Synthesis, and Evaluation of Inhibitors of Trypanosome Growth for Neglected Disease Drug Discovery by : William Gilbert Devine

Download or read book Design, Synthesis, and Evaluation of Inhibitors of Trypanosome Growth for Neglected Disease Drug Discovery written by William Gilbert Devine and published by . This book was released on 2015 with total page 346 pages. Available in PDF, EPUB and Kindle. Book excerpt: Neglected tropical diseases (NTDs) are a global burden affecting the lives of over 1 billion people worldwide. Current chemotherapeutics suffer from a slew of undesirable properties, necessitating new drugs. Target repurposing can greatly accelerate the drug discovery process and avoid much of the financial load, indispensable requirements for NTD drug discovery. This practice has been applied to repurposing known inhibitors of human protein tyrosine kinases for three NTDs: African sleeping sickness, Chagas disease, and leishmaniasis. The first project outlined in this dissertation describes the development and target identification of NEU-321, a ligand efficient inhibitor of Trypanosoma cruzi cytochrome P450 lanosterol 14alpha-demethylase. The second project involves the ongoing optimization of analogs of the repurposed anticancer drug lapatinib against Trypanosoma brucei, T. cruzi, and Leishmania. Scaffold variations of lapatinib has identified key motifs for activity and differentiated leads for the NTDs caused by these protozoan parasites. Enhancement of the physicochemical properties has led to new, more drug-like leads, one of which has shown efficacy in a mouse model of bloodstream T. brucei infection. The third project details our efforts repurposing a larger group of known kinase inhibitors with greater structural diversity. From this campaign was identified NEU-1053, a compound that showed no structural similarity to any other within the screening panel. While highly potent, this compound is not predicted to be brain penetrant, a necessary property to treat late stage African sleeping sickness. This chapter entails our efforts identify important structural parameters for activity, and to improve the predicted brain penetration.

Medicinal Chemistry of Neglected and Tropical Diseases

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Publisher : CRC Press
ISBN 13 : 1351011634
Total Pages : 461 pages
Book Rating : 4.3/5 (51 download)

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Book Synopsis Medicinal Chemistry of Neglected and Tropical Diseases by : Venkatesan Jayaprakash

Download or read book Medicinal Chemistry of Neglected and Tropical Diseases written by Venkatesan Jayaprakash and published by CRC Press. This book was released on 2019-08-15 with total page 461 pages. Available in PDF, EPUB and Kindle. Book excerpt: Medicinal Chemistry of Neglected and Tropical Diseases: Advances in the Design and Synthesis of Antimicrobial Agents consolidates and describes modern drug discovery and development approaches currently employed to identify effective chemotherapeutic agents for the treatment of Neglected Tropical Diseases (NTDs) from a medicinal chemistry perspective. Chapters are designed to cater to the needs of medicinal chemists who work with chemotherapeutic developments for NTDs, as well as serve as a guide to budding medicinal chemists who wish to work in this area. It will introduce rational drug design approaches adopted in designing chemotherapeutics and validated targets available for the purpose.

Discovery and Development of Drugs for Neglected Diseases: Chagas Disease, Human African Trypanosomiasis, and Leishmaniasis

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Publisher : Frontiers Media SA
ISBN 13 : 2889717925
Total Pages : 171 pages
Book Rating : 4.8/5 (897 download)

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Book Synopsis Discovery and Development of Drugs for Neglected Diseases: Chagas Disease, Human African Trypanosomiasis, and Leishmaniasis by : Gildardo Rivera

Download or read book Discovery and Development of Drugs for Neglected Diseases: Chagas Disease, Human African Trypanosomiasis, and Leishmaniasis written by Gildardo Rivera and published by Frontiers Media SA. This book was released on 2021-12-20 with total page 171 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Drug Discovery for Leishmaniasis

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Publisher : Royal Society of Chemistry
ISBN 13 : 1788012585
Total Pages : 422 pages
Book Rating : 4.7/5 (88 download)

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Book Synopsis Drug Discovery for Leishmaniasis by : Luis Rivas

Download or read book Drug Discovery for Leishmaniasis written by Luis Rivas and published by Royal Society of Chemistry. This book was released on 2017-10-26 with total page 422 pages. Available in PDF, EPUB and Kindle. Book excerpt: For human health, leishmaniasis is among the most important protozoan diseases, superseded only by malaria. Globally, 10 to 12 million people are infected with 1.5 million new cases every year. The development of cheaper new drugs is urgently needed for this neglected disease that is developing resistance to current treatments. Chemotherapy remains the only treatment option for the bulk of patients. However, this is largely unaffordable for most. In the past three years numerous advances in drug discovery have been made for treating this disease by exploiting diverging metabolic pathways between the Leishmania enzymes and their hosts, using nanotechnology to target the immune cell phagolysosomes where Leishmania resides. Drug Discovery for Leishmaniasis aims to provide a perspective of the current treatments and their challenges, blended with the emerging strategies and methodologies that will drive new target appraisals and drug developments, as well as addressing the molecular basis of resistance in Leishmania. Recent studies have shown that leishmaniasis affects some of the poorest people in the world, with 95% of fatal cases occurring in only 6 countries. With the WHO goal of eliminating this public health problem in the South-east Asia Region by 2020, this book will be important for anyone who is interested in neglected tropical diseases.

Investing to Overcome the Global Impact of Neglected Tropical Diseases

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Publisher : World Health Organization
ISBN 13 : 9241564865
Total Pages : 211 pages
Book Rating : 4.2/5 (415 download)

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Book Synopsis Investing to Overcome the Global Impact of Neglected Tropical Diseases by : World Health Organization

Download or read book Investing to Overcome the Global Impact of Neglected Tropical Diseases written by World Health Organization and published by World Health Organization. This book was released on 2015-08-05 with total page 211 pages. Available in PDF, EPUB and Kindle. Book excerpt: "The presence, or absence, of neglected tropical diseases (NTDs) can be seen as a proxy for poverty and for the success of interventions aimed at reducing poverty. Today, coverage of the public-health interventions recommended by the World Health Organization (WHO) against NTDs may be interpreted as a proxy for universal health coverage and shared prosperity - in short, a proxy for coverage against neglect. As the world's focus shifts from development to sustainable development, from poverty eradication to shared prosperity, and from disease-specific goals to universal health coverage, control of NTDs will assume an important role towards the target of achieving universal health coverage, including individual financial risk protection. Success in overcoming NTDs is a "litmus test" for universal health coverage against NTDs in endemic countries. The first WHO report on NTDs (2010) set the scene by presenting the evidence for how these interventions had produced results. The second report (2013) assessed the progress made in deploying them and detailed the obstacles to their implementation. This third report analyses for the first time the investments needed to achieve the scale up of implementation required to achieve the targets of the WHO Roadmap on NTDs and universal coverage against NTDs. INVESTING TO OVERCOME THE GLOBAL IMPACT OF NEGLECTED TROPICAL DISEASES presents an investment strategy for NTDs and analyses the specific investment case for prevention, control, elimination and eradication of 12 of the 17 NTDs. Such an analysis is justified following the adoption by the Sixty-sixth World Health Assembly in 2013 of resolution WHA6612 on neglected tropical diseases, which called for sufficient and predictable funding to achieve the Roadmap's targets and sustain control efforts. The report cautions, however, that it is wise investment and not investment alone that will yield success. The report registers progress and challenges and signals those that lie ahead. Climate change is expected to increase the spread of several vector-borne NTDs, notably dengue, transmission of which is directly influenced by temperature, rainfall, relative humidity and climate variability primarily through their effects on the vector. Investments in vector-borne diseases will avoid the potentially catastrophic expenditures associated with their control. The presence of NTDs will thereby signal an early warning system for climate-sensitive diseases. The ultimate goal is to deliver enhanced and equitable interventions to the most marginalized populations in the context of a changing public-health and investment landscape to ensure that all peoples affected by NTDs have an opportunity to lead healthier and wealthier lives."--Publisher's description.

Trypanosomiasis and Leishmaniasis

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Publisher :
ISBN 13 :
Total Pages : 392 pages
Book Rating : 4.:/5 (89 download)

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Book Synopsis Trypanosomiasis and Leishmaniasis by : Geoff Hide

Download or read book Trypanosomiasis and Leishmaniasis written by Geoff Hide and published by . This book was released on 1997 with total page 392 pages. Available in PDF, EPUB and Kindle. Book excerpt: Trypanosomiasis and Leishmaniasis are related diseases caused by single celled organisms (protozoa) transmitted by insects. Between them, these diseases are responsible for much suffering among humans and livestock and so a greater understanding of their biology is a vital part of the campaign to control them. Modern molecular techniques available for use in understanding the control of these diseases are becoming more sophisticated and are increasingly becoming universally applicable to a wide variety of diseases. This book brings together the research approaches that are used interchangeably to understand both Trypanosomiasis and Leishmaniasis. Examples of such fruitful integration can be seen in a number of research areas: genome mapping, molecular and population genetic approaches to epidemiology, studies on polyamine metabolism and possible targets for rational drug design, studies on cellular signalling as a route to understanding host-parasite interactions and studies on chemotherapy and drug resistance. There are also chapters that consider those features that are unique to either Trypanosomiasis or Leishmaniasis. Thus a broad overview of the biology of each disease from the molecular level right up to the whole animal is provided. Contributors come from the leading research groups working on these diseases and include clinicians, laboratory based researchers and social scientists. The book provides an up-to-date summary of the advances in the understanding of these diseases that have come about through the use of modern technologies. By presenting an integration of research into both Trypanosomiasis and Leishmaniasis this book provides an innovative contribution to the literature in this area. It is important reading for all parasitologists, pharmacologists, epidemiologists and clinicians working with these organisms. It is also a useful resource for veterinarians, public health workers, policy makers and social scientists concerned with Trypanosomiasis or Leishmaniasis.

Discovery and Development of Therapeutics from Natural Products Against Neglected Tropical Diseases

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Publisher : Elsevier
ISBN 13 : 0128157240
Total Pages : 458 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis Discovery and Development of Therapeutics from Natural Products Against Neglected Tropical Diseases by : Goutam Brahmachari

Download or read book Discovery and Development of Therapeutics from Natural Products Against Neglected Tropical Diseases written by Goutam Brahmachari and published by Elsevier. This book was released on 2019-04-15 with total page 458 pages. Available in PDF, EPUB and Kindle. Book excerpt: Discovery and Development of Therapeutics from Natural Products against Neglected Tropical Diseases draws together research on medicinal agents from natural sources as starting points for the design of drugs against Neglected Tropical Diseases (NTDs). From the prediction of promising leads and identification of active agents, to the extraction of complex molecules, the book explores novel, economical and efficacious therapeutics for these diseases. It describes current research and the role of natural products, antimalarial compounds from marine natural products and sesquiterpene lactones, natural antileprotic agents, natural products with potential against Leishmaniasis, Trypanosomiasis and Dengue, and more. In addition, Quinoline and Isoquinoline alkaloids for developing new antiprotozoal agents are discussed, alongside anti-trypanosomatid heterocyclic compounds as structures for development. Combining the expertise of specialists from around the world, this volume aims to support and encourage researchers in the investigation of natural sources as starting points for the development of novel, safe and effective agents for use against neglected tropical diseases. Includes chapters written by active researchers and leading global experts deeply engaged in the research field of natural product chemistry for drug discovery Draws together cutting-edge research advances in natural product chemistry that are targeted at neglected tropical diseases Highlights the future potential of natural products as sources of novel medicinal compounds against neglected tropical diseases

Chemical Epigenetics

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Publisher : Springer Nature
ISBN 13 : 3030429822
Total Pages : 569 pages
Book Rating : 4.0/5 (34 download)

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Book Synopsis Chemical Epigenetics by : Antonello Mai

Download or read book Chemical Epigenetics written by Antonello Mai and published by Springer Nature. This book was released on 2020-03-31 with total page 569 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents an authoritative review of the most significant findings about all the epigenetic targets (writers, readers, and erasers) and their implication in physiology and pathology. The book also covers the design, synthesis and biological validation of epigenetic chemical modulators, which can be useful as novel chemotherapeutic agents. Particular attention is given to the chemical mechanisms of action of these molecules and to the drug discovery prose which allows their identification. This book will appeal to students who want to know the extensive progresses made by epigenetics (targets and modulators) in the last years from the beginning, and to specialized scientists who need an instrument to quickly search and check historical and/or updated notices about epigenetics.

The Microbiology of Central Nervous System Infections

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Publisher : Academic Press
ISBN 13 : 0128138076
Total Pages : 348 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis The Microbiology of Central Nervous System Infections by :

Download or read book The Microbiology of Central Nervous System Infections written by and published by Academic Press. This book was released on 2018-02-17 with total page 348 pages. Available in PDF, EPUB and Kindle. Book excerpt: The Microbiology of Central Nervous System Infections, Volume 3, discusses modern approaches to the diagnosis, treatment and prophylaxis of central nervous system (CNS) infections. This new release is divided into five sections that cover treatment strategies, imaging, molecular diagnosis, management of CNS infections with metal nanoparticles, and prophylaxis of CNS infections, including bacterial, viral and fungal infections. The last section contains a chapter on transmissible spongiform encephalopathies and modern trends in its diagnosis and treatment. University teachers, medical practitioners, graduate and postgraduate students, researchers in microbiology, and those in the pharmaceutical and laboratory diagnostic industries will find the book very important. Encompasses a broad range of central nervous system infections, including questions of etiology, pathogenesis, diagnosis, prognosis, treatment and prophylaxis Written by highly professional and eminent surgeons, microbiologists and infectious disease specialists Includes scientific understanding and practical guidelines, making it interesting for both research scientists and practitioners

Third World Diseases

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Publisher : Springer Science & Business Media
ISBN 13 : 3642234879
Total Pages : 321 pages
Book Rating : 4.6/5 (422 download)

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Book Synopsis Third World Diseases by : Richard L. Elliott

Download or read book Third World Diseases written by Richard L. Elliott and published by Springer Science & Business Media. This book was released on 2011-09-01 with total page 321 pages. Available in PDF, EPUB and Kindle. Book excerpt: Federico Gomez de las Heras: Overview of Neglected Tropical Diseases Gwendolyn A. Marriner Amit Nayyar, Eugene Uh, Sharon Y. Wong, Tathagata Mukherjee, Laura E. Via , Matthew Carroll, Rachel L. Edwards, Todd D. Gruber, Inhee Choi, Jinwoo Lee, Kriti Arora, Kathleen D. England, Helena I.M. Boshoff, Clifton E. Barry III: The Medicinal Chemistry of Tuberculosis Chemotherapy Jeremy N. Burrows, David Waterson: Discovering New Medicines to Control and Eradicate Malaria Tomas von Geldern, Michael Oscar Harhay, Ivan Scandale, Robert Don: Kinetoplastid Parasites Pei-Yong Shi,, Zheng Yin, Shahul Nilar, Thomas H. Keller: Dengue Drug Discovery Dan Marquess: Recent Advances in Discovery and Development of Medicines for the Treatment of Secretory Diarrhea in the Developing World

Fragment-based Approaches in Drug Discovery

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Publisher : John Wiley & Sons
ISBN 13 : 3527608605
Total Pages : 391 pages
Book Rating : 4.5/5 (276 download)

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Book Synopsis Fragment-based Approaches in Drug Discovery by : Wolfgang Jahnke

Download or read book Fragment-based Approaches in Drug Discovery written by Wolfgang Jahnke and published by John Wiley & Sons. This book was released on 2006-12-13 with total page 391 pages. Available in PDF, EPUB and Kindle. Book excerpt: This first systematic summary of the impact of fragment-based approaches on the drug development process provides essential information that was previously unavailable. Adopting a practice-oriented approach, this represents a book by professionals for professionals, tailor-made for drug developers in the pharma and biotech sector who need to keep up-to-date on the latest technologies and strategies in pharmaceutical ligand design. The book is clearly divided into three sections on ligand design, spectroscopic techniques, and screening and drug discovery, backed by numerous case studies.

The Role of Natural Products in Drug Discovery

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Publisher : Springer Science & Business Media
ISBN 13 : 3662040425
Total Pages : 363 pages
Book Rating : 4.6/5 (62 download)

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Book Synopsis The Role of Natural Products in Drug Discovery by : J. Mulzer

Download or read book The Role of Natural Products in Drug Discovery written by J. Mulzer and published by Springer Science & Business Media. This book was released on 2013-04-17 with total page 363 pages. Available in PDF, EPUB and Kindle. Book excerpt: Natural Products have been important sources of useful drugs from prehistoric times to the present. This book gives an overview about this field and provides important recent contributions to the discovery of new drugs generated by research on natural products. Total synthesis of natural products with interesting biological activities is paving the way for the preparation of new and improved analogs. The methods of combinatorial chemistry permit the selection of the best drug from a large number of candidates. Beyond synthesis and evaluation of organic molecules a number of new bioorganic methods are coming to the fore and will be discucced in this isue of the ERnst schering Research Foundation workshop proceedings.

Global Tuberculosis Report 2017

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Publisher : World Health Organization
ISBN 13 : 9789241565516
Total Pages : 0 pages
Book Rating : 4.5/5 (655 download)

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Book Synopsis Global Tuberculosis Report 2017 by : World Health Organization

Download or read book Global Tuberculosis Report 2017 written by World Health Organization and published by World Health Organization. This book was released on 2017-12-13 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: WHO's Global Tuberculosis Report provides a comprehensive and up-to-date assessment of the TB epidemic and of progress in care and prevention at global, regional and country levels. This is done in the context of recommended global TB strategies and associated targets, and broader development goals. For the period 2016-2035, these are WHO's End TB Strategy and the United Nations' (UN) Sustainable Development Goals (SDGs), which share a common aim: to end the global TB epidemic. The main data sources for the report are annual rounds of global TB data collection implemented by WHO's Global TB Program since 1995 and databases maintained by other WHO departments, UNAIDS and the World Bank. In WHO's 2017 round of global TB data collection, 201 countries and territories that account for over 99% of the world's population and TB cases reported data.

Approaches to Design and Synthesis of Antiparasitic Drugs

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Publisher : Elsevier
ISBN 13 : 0080527523
Total Pages : 525 pages
Book Rating : 4.0/5 (85 download)

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Book Synopsis Approaches to Design and Synthesis of Antiparasitic Drugs by : N. Anand

Download or read book Approaches to Design and Synthesis of Antiparasitic Drugs written by N. Anand and published by Elsevier. This book was released on 1997-07-10 with total page 525 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents a comprehensive and up to date account of the chemotherapy of parasitic diseases, both human and veterinary. The book starts with an overview of parasitic diseases. The body of the book is divided into two parts: antihelminthic drugs, and antiprotozoal drugs. Both parts start with chapters highlighting the 'biochemical targets' available for chemotherapeutic interference. Individual chapters deal with one chemical class of compounds and describe their origin, structure-activity relationship, mode of action, and methods of synthesis and their status both in clinical and veterinary practice. The book will be useful to a wide spectrum of readers: students embarking on a research career in parasitic chemotherapy, clinicians (and veterinarians) and clinical pharmacologists desiring detailed information about the drugs currently in use, and pharmaceutical technologists wanting to update their knowledge of the methods of manufacture.

Recent Advances in the Synthesis of Organic Compounds to Combat Neglected Tropical Diseases

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Publisher : Bentham Science Publishers
ISBN 13 : 1608059022
Total Pages : 285 pages
Book Rating : 4.6/5 (8 download)

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Book Synopsis Recent Advances in the Synthesis of Organic Compounds to Combat Neglected Tropical Diseases by : Adilson Beatriz

Download or read book Recent Advances in the Synthesis of Organic Compounds to Combat Neglected Tropical Diseases written by Adilson Beatriz and published by Bentham Science Publishers. This book was released on 2014-08-04 with total page 285 pages. Available in PDF, EPUB and Kindle. Book excerpt: The World Health Organization (WHO) has reported 14 diseases that are occurring exclusively in tropical areas. Most of these diseases are infectious and mainly affect poor populations. Some of these diseases include malaria, dengue fever, leishmaniasis and Chagas disease. Therefore, an acute need for increasing the arsenal of drugs is required to fight against these neglected diseases for the guaranteed recovery and relief of many patients. This E-book gathers important scientific research performed by scientists worldwide showing the state of the art of Medicinal Chemistry dedicated to the synthesis of compounds that are potentially bioactive against the causative agents of neglected diseases. The contents of this book include chapters on recent advances in synthetic organic compounds for the prevention of Chagas disease, recent advances in the discovery of small organic molecules for the prevention and treatment of dengue fever, leishmaniasis, leprosy, therapeutic arsenal and drug discovery for lymphatic filariasis, therapeutic agents for the treatment of malaria, schistosomiasis and synthetic organic compounds as potential antitubercular drugs. This book is intended for undergraduate and graduate students in institutes, colleges, universities and academies who want to specialize in the field of organic synthesis and medicinal chemistry.This book will also be a valuable resource of information for researchers in this field.

Promoting Access to Medical Technologies and Innovation - Intersections between Public Health, Intellectual Property and Trade

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Publisher : WIPO
ISBN 13 : 9280523082
Total Pages : 259 pages
Book Rating : 4.2/5 (85 download)

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Book Synopsis Promoting Access to Medical Technologies and Innovation - Intersections between Public Health, Intellectual Property and Trade by : World Intellectual Property Organization

Download or read book Promoting Access to Medical Technologies and Innovation - Intersections between Public Health, Intellectual Property and Trade written by World Intellectual Property Organization and published by WIPO. This book was released on 2013 with total page 259 pages. Available in PDF, EPUB and Kindle. Book excerpt: This study has emerged from an ongoing program of trilateral cooperation between WHO, WTO and WIPO. It responds to an increasing demand, particularly in developing countries, for strengthened capacity for informed policy-making in areas of intersection between health, trade and IP, focusing on access to and innovation of medicines and other medical technologies.

Handbook of Animal Models of Infection

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Publisher : Academic Press
ISBN 13 : 0080533558
Total Pages : 1169 pages
Book Rating : 4.0/5 (85 download)

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Book Synopsis Handbook of Animal Models of Infection by : Merle A. Sande

Download or read book Handbook of Animal Models of Infection written by Merle A. Sande and published by Academic Press. This book was released on 1999-05-28 with total page 1169 pages. Available in PDF, EPUB and Kindle. Book excerpt: Handbook of Animal Models of Infection is a complete revision of a three-volume text that was published in 1986. It incorporates the major advances in the field during the past decade, in particular those concerning molecular biological procedures and new models that have been developed. It focuses on both methods and techniques, which makes it an essential and comprehensive reference as well as a benchtop manual. The Handbook will help investigators save time and effort in formulating an approach to test a new potential therapeutic agent or combination of agents for in vivo efficacy and to position the therapy for specific infections where it may have therapeutic promise. The book is divided into five sections; the first covering the general methodologies, followed by sections describing experimental bacterial, mycotic, parasitic, and viral infections. - Discusses ethical and safety aspects in an introductory background section - Covers principles of animal care and current techniques appropriate for the use of animal models of infection - Details a wide range of animals including rodents, rabbits, cats, and primates - Provides hands-on descriptions of how to set up the model - Discusses the major advantages and limitations of each model - Ensures full coverage of bacterial, fungal, viral, and parasitic infections