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


by

Adilson Beatriz, Dênis Pires de Lima

DOI: 10.2174/97816080590271140101
eISBN: 978-1-60805-902-7, 2014
ISBN: 978-1-60805-903-4



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The World Health Organization (WHO) has reported 14 diseases that are occurring exclusively in tropical areas. Most of these diseases ...[view complete introduction]

Table of Contents

Foreword

- Pp. i

Carolina Horta Andrade

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Preface

- Pp. ii

Adilson Beatriz and Dênis Pires de Lima

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List of Contributors

- Pp. iii-v (3)

Adilson Beatriz and Dênis Pires de Lima

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CHAGAS DISEASE An Overview of Recent Advances in the Search for Synthetic Organic Compounds with Trypanocidal Activity

- Pp. 3-31 (29)

Ana Camila Micheletti, Edson dos Anjos dos Santos and Felicia Megumi Ito

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DENGUE FEVER Recent Advances in the Discovery of Small Organic Molecules for the Prevention and Treatment of Dengue Fever

- Pp. 32-62 (31)

Lucas Cunha Dias de Rezende, Victor Hugo Aquino and Flavio da Silva Emery

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LEISHMANIASIS An Overview of New Synthetic Antileishmanial Candidates

- Pp. 63-121 (59)

Nubia Boechat and Luiz Carlos da Silva Pinheiro

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LEPROSY Chasing Potential Antileprotic Compounds

- Pp. 122-148 (27)

Dênis Pires de Lima and Davidson Pires de Lima

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LYMPHATIC FILARIASIS Therapeutic Arsenal and Drug Discovery for Lymphatic Filariasis from a Synthetic Point of View

- Pp. 149-171 (23)

Gabriela Bianchi dos Santos, Ana Patrícia Yatsuda Natsui and Flavio da Silva Emery

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MALARIA Synthesis of Hybrid Molecules and Inhibitors of Falcipain for Use as Therapeutic Agents in Treatment of Malaria

- Pp. 172-195 (24)

Renata Barbosa de Oliveira, Marcela Silva Lopes and Saulo Fehelberg Pinto Braga

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SCHISTOSOMIASIS Recent Progresses in Synthesis and Evaluation of Bioactive Compounds with Molluscicidal Activity - Molluscicidal Activity of Synthetic and Natural Products

- Pp. 196-230 (35)

Ronaldo Nascimento de Oliveira and Ricardo A. W. Neves Filho

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TUBERCULOSIS Synthetic Organic Compounds as Potential Antitubercular Drugs: A Review of the Progress Made in the Last Five Years

- Pp. 231-266 (36)

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

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Subject Index

- Pp. 267-276 (10)

Adilson Beatriz and Dênis Pires de Lima

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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 approved that targeted NTDs. Fortunately, over the past decade the tide has began to turn, 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


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. Nowadays, 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

List of Contributors

Editor(s):
Adilson Beatriz
Federal University of Mato Grosso do Sul
Brazil


Dênis Pires de Lima
Federal University of Mato Grosso do Sul
Brazil




Contributor(s):
Aquino Vitor Hugo
Department of Clinical
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
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


Fernandes Guilherme F. dos Santos
Faculty of Pharmaceutical Sciences
Paulista State University- UNESP
Araraquara-SP
Brazil


Ito Felicia Megumi
Federal Institute of Mato Grosso do Sul.
Rua Tanure Salime
Coxim-MS
s/n, 79400-000
Brazil


Leite Clarice Q. F.
Laboratory of Mycobacteriology “Prof. Dr. Hugo David”
Department of Biological Science
Faculty of Pharmaceutical Sicences
Paulista State University
UNESP
Jaú-SP
Brazil


Lopes Marcela Silva
Laboratory of Pharmaceutical Chemistry
Faculty of Pharmacy
Federal University of Minas Gerais
Belo Horizonte-MG
Brazil


Marino Leonardo B.
Laboratory of Mycobacteriology “Prof. Dr. Hugo David”
Department of Biological Science
Faculty of Pharmaceutical Sicences
Paulista State University
UNESP
Jaú-SP
Brazil


Micheletti Ana Camila
Institute of Chemistry
Federal University of Mato Grosso do Sul
Campo Grande-MS
Brazil


Natsui Ana Patricia Yatsuda
Department of Clinical
Toxicological and Bromatological Analyses
Faculty of Pharmaceutical Sciences of Ribeirao Preto
São Paulo University- USP
Ribeirão Preto-SP
Brazil


Neves Filho Ricardo A.W.
Department of Bioorganic Chemistry
Leibniz Institute of Plant Biochemistry
São Paulo University- USP
Weinberg
Germany


Oliveira Renata Barbosa de
Laboratory of Pharmaceutical Chemistry
Faculty of Pharmacy
Federal University of Minas Gerais
Belo Horizonte-MG
Brazil


Oliveira Ronaldo Nascimento de
Laboratory of Synthesis of Bioactive Compounds
Department of Molecular Sciences
Federal Rural University of Pernambuco
Recife-PE
Brazil


Pavan Fernando Rogério
Laboratory of Mycobacteriology “Prof. Dr. Hugo David”
Department of Biological Science
Faculty of Pharmaceutical Sicences
Paulista State University
UNESP
Jaú-SP
Brazil


Pinheiro Luiz Carlos da Silva
Department of Organic Synthesis
Institute of Drug Technology - Farmanguinhos
Oswaldo Cruz Foundation- Fiocruz
Paulista State University
Rio de Janeiro-RJ
Brazil


Rezende Lucas Cunha Dias
Department of Pharmaceutical Sciences
Faculty of Pharmaceutical Sciences of Riberão Preto – FCFRP
University of São Paulo
Paulista State University- USP
Ribeirao Preto – SP
Brazil


Santos Edson dos Anjos dos
Federal Technological University of Paraná
Apucarana-PR
Brazil


Santos Edson dos Anjos dos
Federal Technological University of Paraná
Apucarana-PR
Brazil


Santos Gabriela Bianchi dos
Department of Pharmaceutical Sciences
Faculty of Pharmaceutical Sciences of Ribeirão Preto - FCFRP
São Paulo University - USP
Ribeirão Preto-SP
Brazil


Santos Jean Leandro
Faculty of Pharmaceutical Sciences
Paulista State University- UNESP
Araraquara-SP
Brazil




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