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Experimental Chemotherapy for Chagas Disease : A Morphological, Biochemical, and Proteomic Overview of Potential Trypanosoma cruzi Targets of Amidines Derivatives and Naphthoquinones
Joint Authors
Batista, Wanderson
Oliveira, Gabriel M.
Soeiro, Maria de Nazaré C.
de Castro, Solange Lisboa
Batista, Denise G. J.
Silva, Cristiane F.
de Souza, Elen M.
Menna-Barreto, Rubem F. S.
Batista, Marcos M.
Silva, Patricia B.
Daliry, Anissa
Salomão, Kelly
Source
Molecular Biology International
Issue
Vol. 2011, Issue 2011 (31 Dec. 2011), pp.1-13, 13 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2011-06-30
Country of Publication
Egypt
No. of Pages
13
Main Subjects
Natural & Life Sciences (Multidisciplinary)
Biology
Abstract EN
Chagas disease (CD), caused by Trypanosoma cruzi, affects approximately eight million individuals in Latin America and is emerging in nonendemic areas due to the globalisation of immigration and nonvectorial transmission routes.
Although CD represents an important public health problem, resulting in high morbidity and considerable mortality rates, few investments have been allocated towards developing novel anti-T.
cruzi agents.
The available therapy for CD is based on two nitro derivatives (benznidazole (Bz) and nifurtimox (Nf)) developed more than four decades ago.
Both are far from ideal due to substantial secondary side effects, limited efficacy against different parasite isolates, long-term therapy, and their well-known poor activity in the late chronic phase.
These drawbacks justify the urgent need to identify better drugs to treat chagasic patients.
Although several classes of natural and synthetic compounds have been reported to act in vitro and in vivo on T.
cruzi, since the introduction of Bz and Nf, only a few drugs, such as allopurinol and a few sterol inhibitors, have moved to clinical trials.
This reflects, at least in part, the absence of well-established universal protocols to screen and compare drug activity.
In addition, a large number of in vitro studies have been conducted using only epimastigotes and trypomastigotes instead of evaluating compounds' activities against intracellular amastigotes, which are the reproductive forms in the vertebrate host and are thus an important determinant in the selection and identification of effective compounds for further in vivo analysis.
In addition, due to pharmacokinetics and absorption, distribution, metabolism, and excretion characteristics, several compounds that were promising in vitro have not been as effective as Nf or Bz in animal models of T.
cruzi infection.
In the last two decades, our team has collaborated with different medicinal chemistry groups to develop preclinical studies for CD and investigate the in vitro and in vivo efficacy, toxicity, selectivity, and parasite targets of different classes of natural and synthetic compounds.
Some of these results will be briefly presented, focusing primarily on diamidines and related compounds and naphthoquinone derivatives that showed the most promising efficacy against T.
cruzi.
American Psychological Association (APA)
de Castro, Solange Lisboa& Batista, Denise G. J.& Batista, Marcos M.& Batista, Wanderson& Daliry, Anissa& de Souza, Elen M.…[et al.]. 2011. Experimental Chemotherapy for Chagas Disease : A Morphological, Biochemical, and Proteomic Overview of Potential Trypanosoma cruzi Targets of Amidines Derivatives and Naphthoquinones. Molecular Biology International،Vol. 2011, no. 2011, pp.1-13.
https://search.emarefa.net/detail/BIM-462101
Modern Language Association (MLA)
de Castro, Solange Lisboa…[et al.]. Experimental Chemotherapy for Chagas Disease : A Morphological, Biochemical, and Proteomic Overview of Potential Trypanosoma cruzi Targets of Amidines Derivatives and Naphthoquinones. Molecular Biology International No. 2011 (2011), pp.1-13.
https://search.emarefa.net/detail/BIM-462101
American Medical Association (AMA)
de Castro, Solange Lisboa& Batista, Denise G. J.& Batista, Marcos M.& Batista, Wanderson& Daliry, Anissa& de Souza, Elen M.…[et al.]. Experimental Chemotherapy for Chagas Disease : A Morphological, Biochemical, and Proteomic Overview of Potential Trypanosoma cruzi Targets of Amidines Derivatives and Naphthoquinones. Molecular Biology International. 2011. Vol. 2011, no. 2011, pp.1-13.
https://search.emarefa.net/detail/BIM-462101
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-462101