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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5732_Библиотеки_им_академика_М_И_Перельмана
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Recent Advances in the Synthesis of
Organic Compounds to Combat
Neglected Tropical Diseases
Edited By
Adilson Beatriz & Dênis Pires de Lima
Institute of Chemistry
Federal University of Mato Grosso do Sul
Campo Grande, MS
Brazil
Recent Advances in the Synthesis
of Organic Compounds to Combat
Neglected Tropical Diseases
Editor(s) : Adilson Beatriz, Dênis Pires de Lima
ISBN: 978-1-60805-903-4 (Print)
ISBN: 978-1-60805-902-7 (Online)
Year of Publication: 2014
DOI: 10.2174/9781608059027114010
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DEDICATION
This book is dedicated to those who suffered and are still suffering
from neglected diseases. Equally, it is devoted to researchers that with
the commitment to their work routinely contribute by seeking, in many
and different ways, for new drugs to treat those diseases.
CONTENTS
Foreword i
Preface ii
List of Contributors iii
CHAPTERS
1. CHAGAS DISEASE 3
An Overview of Recent Advances in the Search for Synthetic
Organic Compounds with Trypanocidal Activity
Ana Camila Micheletti, Edson dos Anjos dos Santos and Felicia
Megumi Ito
2. DENGUE FEVER 32
Recent Advances in the Discovery of Small Organic Molecules for
the Prevention and Treatment of Dengue Fever
Lucas Cunha Dias de Rezende, Victor Hugo Aquino and Flavio da
Silva Emery
3. LEISHMANIASIS 63
An Overview of New Synthetic Antileishmanial Candidates
Nubia Boechat and Luiz Carlos da Silva Pinheiro
4. LEPROSY 122
Chasing Potential Antileprotic Compounds
Dênis Pires de Lima and Davidson Pires de Lima
5. LYMPHATIC FILARIASIS 149
Therapeutic Arsenal and Drug Discovery for Lymphatic Filariasis
from a Synthetic Point of View
Gabriela Bianchi dos Santos, Ana Patrícia Yatsuda Natsui and
Flavio da Silva Emery
6. MALARIA 172
Synthesis of Hybrid Molecules and Inhibitors of Falcipain for Use
as Therapeutic Agents in Treatment of Malaria
Renata Barbosa de Oliveira, Marcela Silva Lopes and Saulo
Fehelberg Pinto Braga
7. SCHISTOSOMIASIS 196
Recent Progresses in Synthesis and Evaluation of Bioactive
Compounds with Molluscicidal Activity - Molluscicidal Activity of
Synthetic and Natural Products
Ronaldo Nascimento de Oliveira and Ricardo A. W. Neves Filho
8. TUBERCULOSIS 231
Synthetic Organic Compounds as Potential Antitubercular Drugs:
A Review of the Progress Made in the Last Five Years
Jean Leandro Santos, Guilherme F. dos Santos Fernandes, Priscila
Longhin Bosquesi, Leonardo B. Marino, Clarice Q. F. Leite, Chung
M. Chin and Fernando Rogério Pavan
Subject Index 267
i
FOREWORD
Half the disease burden of the developing world – 80% of the world’s population –
is due to infectious and parasitic diseases, most of which are preventable and/or
treatable. More than 1 billion people is affected by at least one neglected tropical
diseases (NTDs), primarily poor populations living in tropical and subtropical
climates, with an approximated 534 000 deaths per year. These diseases have a huge
impact on labor productivity and costs low-income countries billion of dollars a
year, keeping up the vicious circle of poverty. Yet despite these alarming numbers ,
between 1975 and 1999 only thirteen new drugs were appr oved that targeted NTDs.
Fortunately, over the past decade the tide has began to tur n, in both recognizing the
lack of new medicines dedicated to the diseases of the most neglected populations
and in initiating efforts to redress the problem. In recent years, there has been a
remarkable commitment on the part of ministries of health in endemic countries,
global health initiatives, funding agencies and philanthropists escalated, as did
donations of medicines from pharmaceutical companies and the engagement of the
scientific community, having efforts towards the infectious diseases of the
developing world. In this scenario, medicinal and synthetic chemists are of upmost
importance, for designing, synthetizing and evaluating new drug candidates for
parasitic and infectious diseases. This eBook is dedicated to the theme of “Recent
Advances in the Synthesis of Organic Compounds to Combat Neglected Tropical
Diseases” and features contributions from a Brazilian team of synthetic chemists and
pharmaceutical researchers that work in the field of synthesis of compounds that are
potentially bioactive against the causative agents of NTDs.
Carolina Horta Andrade
LabMol - Laboratory for Molecular Modeling and Drug Design
Faculdade de Farmácia
Universidade Federal de Goiás
Rua 240, Qd. 87
Setor Leste Universitário, 74605-170
Goiânia - GO
Brazil
ii
PREFACE
In the website of WHO, 14 diseases are reported to occur exclusively or specially in
tropics. Most of them are infectious diseases affecting mainly poor populations and
include leishmaniosis, dengue fever, malaria and Chagas disease. These diseases
affect around 1 billion people and, according to WHO, 100% of developing
countries are affected by at least five of these diseases. Accordingly, there is an
urgent necessity for increasing the arsenal of drugs to combat neglected diseases in
order to guarantee relief and well-being to many patients. The situation requires
powerful research and improvement of politics to support investigation in this area
of knowledge. There is a great volume of scientific work dealing with biology,
immunology and genetics of parasites which cause these diseases. Taking in account
the present situation, the role of Organic Chemistry in the pharmaceutical industry
continues to be one of the main propellers for the discovery of new drugs. Medicinal
organic chemists have contributed by seeking new bioactive compounds. Nowada ys,
there is a considerable global effort to evoke awareness to this problem and
overcome the persisting inequality in the focus of drug discovery. Therefore, this
eBook gathers important scientific research performed by scientists worldwide
showing the state of the art of Organic Medicinal Chemistry dedicated to the
synthesis of compounds that are potentially bioactive against the causative agents of
neglected diseases. The eBook intends to be a valuable source of information to
researchers in the area of Medicinal Chemistry, Organic Synthesis, as well as to
undergraduate and graduate students interested in this subject.
The eBook is composed of eight chapters, each of which is dedicated to one type
of neglected disease. Essentially, the authors compiled important work concerning
the synthesis and biological evaluation, according to their targets, of lead
compounds in the process of developing new pharmaceuticals.
Adilson Beatriz
&
Dênis Pires de Lima
Institute of Chemistry
Federal University of Mato Grosso do Sul
Campo Grande – MS
Brazil
iii
List of Contributors
Aquino, Vitor Hugo
Department of Clinical, Toxicological and Bromatological Analysis, Faculty of
Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirao
Preto – SP, Brazil
Boechat, Nubia
Department of Organic Synthesis, Institute of Drug Technology - Farmanguinhos,
Oswaldo Cruz Foundation - Fiocruz, Rio de Janeiro-RJ, Brazil
Bosquesi, Priscila Longhin
Faculty of Pharmaceutical Sciences, Paulista State University- UNESP,
Araraquara-SP, Brazil
Braga, Saulo Fehelberg Pinto
Laboratory of Pharmaceutical Chemistry, Faculty of Pharmacy, Federal
University of Minas Gerais, Belo Horizonte-MG, Brazil
Chin, Chung M.
Departamento de Fármacos e Medicamentos, Faculty of Pharmaceutical
Sciences, Paulista State University- UNESP, Araraquaara-SP, Brazil
de Lima, Davidson Pires
Department of Clinical Medicine, Faculty of Medicine, Federal University of
Minas Gerais, Belo Horizonte-MG, Brazil
de Lima, Dênis Pires
Institute of Chemistry, Federal University of Mato Grosso do Sul, Campo
Grande-MS, Brazil
Emery, Flávio da Silva
Department of Pharmaceutical Sciences, Faculty of Pharmaceutical Sciences of
Ribeirão Preto – FCFRP, University of São Paulo - USP, Ribeirao Preto – SP,
Brazil
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