Progress in the research of artemisinin-related antimalarials: An update

Woerdenbag, Herman J.; Pras, Niesko; Uden, W van; Wallaart, Thorvald; Beekman, Aäron C.; Lugt, C.

doi:10.1007/bf01872865

Cited by 82 publications

(53 citation statements)

References 127 publications

(90 reference statements)

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“…The renewed interest in both natural and semisynthetic endoperoxides and NO-containing products, both of which present interesting medicinal applications [1][2][3][4][5] , led us to reconsider the preparation of these structures through DielsAlder reactions. Heteroatomic functional arrangements can result in dienophiles which react to produce heterocyclic Diels-Alder adducts 6,7 .…”

Section: Introductionmentioning

confidence: 99%

Hetero Diels-Alder adduct formation between nitrosobenzene and tetra-methyl purpurogallin and its retro-Diels-Alder reaction

Gamenara¹,

Dias²,

Tancred³

et al. 2001

J. Braz. Chem. Soc.

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É descrita uma síntese eficiente de um aduto de Diels-Alder da tetrametilpurpurogalina (TMPG) e o nitrosobenzeno (NOB). A cinética da decomposição térmica do aduto, que segue um mecanismo de retro-Diels-Alder foi estudada usando espectroscopía de 1 H-RMN.An efficient synthesis of a Diels-Alder adduct between purpurogallin tetramethyl ether (TMPG) and nitrosobenzene (NOB) is reported. The thermal decomposition kinetics of the adduct, which follows a retro-Diels-Alder mechanism, was studied using 1 H-NMR spectroscopy.

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Section: Introductionmentioning

confidence: 99%

Hetero Diels-Alder adduct formation between nitrosobenzene and tetra-methyl purpurogallin and its retro-Diels-Alder reaction

Gamenara¹,

Dias²,

Tancred³

et al. 2001

J. Braz. Chem. Soc.

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“…This agent also provokes hemolysis, which could be due to accelerated oxidative denaturation of haemoglobin, and lipid per oxidation associated with decreased GSH. Endoperoxide-containing compounds, such as epidioxy-A 7 -octalin, may also act through the production of oxidative stress (Buffinton ET AL., 1986;Vennerstrom & Eaton, 1988 Posner ET AL, 1994;Woerdenbag ET AL, 1994).…”

Section: Antimalarial Effects Of Prooxidantsmentioning

confidence: 99%

Recent developments and rationale towards new strategies for malarial chemotherapy

Vial¹

1996

Parasite

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Summary :The major problem facing world research for new antimalarials lies in encountered difficulties in the search for new promising paths. The past 20 years have witnessed a very impressive increase in our understanding of the biochemistry and molecular biology of malaria parasites, with attention focused on specific parasite molecules that are keys to the parasite life cycle or the induction of its pathogenesis. Directed pharmacology research has involved the identification and characterization of targets that can be specifically pharmacologically affected, including the replicating machinery of the parasites, various metabolisms such as the purine salvage pathway, and biosynthesis of pyrimidines or phospholipids. Protease inhibitors (e.g. those degrading haemoglobin], the use of iron chelators or inhibition of heme polymerization, induction of oxidative stress or inhibition of antioxidant enzymes are also investigated. Some pathways have already been validated with current antimalarials but, due to the development of resistance, complete characterization of the molecular structure of the target should allow attack of these exceptional molecules at novel and distinct sites with new drug concepts. The problem in the quest to develop new antimalarials is the fact that the results are not being materialized, but there is no lack of pharmacological targets.

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“…Artesunate (hereafter ARS) is the most frequently used artemisinin derivative, and is rapidly and almost entirely converted to dihydroartemisinin (hereafter DHA) in vivo, mostly by plasma esterases and liver cytochrome P450 CYP2A6 [12][13][14]. DHA is the most active of all artemisinin derivatives, with activity approximately 1.4 times that of ARS [15].…”

Section: Introduction E15mentioning

confidence: 99%

Reprint of “Pharmacokinetic modelling of the anti-malarial drug artesunate and its active metabolite dihydroartemisinin”

Hall

Chappell

Aston

et al. 2014

Computer Methods and Programs in Biomedicine

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c o m p u t e r m e t h o d s a n d p r o g r a m s i n b i o m e d i c i n e 1 1 4 ( 2 0 1 4 ) e14-e28 j o u r n a l h o m e p a g e : w w w . i n t l . e l s e v i e r h e a l t h . c o m / j o u r n a l s / c m p bReprint of "Pharmacokinetic modelling of the anti-malarial drug artesunate and its active metabolite dihydroartemisinin" r t i c l e i n f oArticle history: Initial validation of the model under various combinations of the constraints leading to identifiable model structures was performed against a dataset of artesunate and dihydroartemisinin concentration-time profiles of 19 malaria patients. When all the discussed constraints were imposed on the model, the resulting globally identifiable model structure was found to fit reasonably well to those patients with normal drug absorption profiles.However, there is wide variability in the fitted parameters and further investigation is warranted.

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Progress in the research of artemisinin-related antimalarials: An update

Cited by 82 publications

References 127 publications

Hetero Diels-Alder adduct formation between nitrosobenzene and tetra-methyl purpurogallin and its retro-Diels-Alder reaction

Hetero Diels-Alder adduct formation between nitrosobenzene and tetra-methyl purpurogallin and its retro-Diels-Alder reaction

Recent developments and rationale towards new strategies for malarial chemotherapy

Reprint of “Pharmacokinetic modelling of the anti-malarial drug artesunate and its active metabolite dihydroartemisinin”

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