Recent Advances in Malaria Chemotherapy

Robert, Anne; Dechy‐Cabaret, Odile; Cazelles, Jérôme; Benoit‐Vical, Françoise; Meunier, Bernard

doi:10.1002/jccs.200200046

Cited by 9 publications

(4 citation statements)

References 85 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…This allows any emerging new products can be priced solely on the basis of manufacturing costs, thus delivering affordable medicines to the people most in need [90]. However, there are numerous other ongoing antimalarial discovery projects which have been the subject of various reviews [42,[91][92][93][94][95][96][97].…”

Section: Fuelling the Development Pipeline -Dis-covery Projectsmentioning

confidence: 99%

The State of the Art in Anti-Malarial Drug Discovery and Development

Burrows

Chibale²,

Wells

2011

CTMC

145

View full text Add to dashboard Cite

Malaria is one of the most prevalent and devastating infectious diseases of our time. Yet, unfortunately, apart from artemisinin combination therapies there are relatively few effective treatments for Plasmodium falciparum and only one treatment for the radical cure of Plasmodium vivax. Novel classes of antimalarial medicines are urgently needed given the long-term inevitability of resistance to current therapies and the need for drugs that are well tolerated by all. This review summarises the antimalarials developed and registered thus far, as well as describing some of the new small molecule therapy approaches being developed as a contribution towards the malaria eradication agenda.

show abstract

Section: Fuelling the Development Pipeline -Dis-covery Projectsmentioning

confidence: 99%

The State of the Art in Anti-Malarial Drug Discovery and Development

Burrows

Chibale²,

Wells

2011

CTMC

145

View full text Add to dashboard Cite

show abstract

“…Trioxaquine 51, the best of these, was only 2-fold less potent than 1. Although no in vivo data has been disclosed for 51, it was claimed 12,22 that trioxaquines are active when administered orally in infected mice. Figure 15: It was fairly early 41 established that simple synthetic acyclic hydroperoxides, peroxyacids, peroxyesters, peroxides, peroxyacetals, and peroxycarbonates are much less potent than 1 and are devoid of activity in vivo.…”

mentioning

confidence: 99%

Synthetic peroxides as antimalarials

Tang

Dong²,

Vennerstrom³

2004

Medicinal Research Reviews

258

123

View full text Add to dashboard Cite

The discovery of artemisinin in 1971 initiated a new era in antimalarial chemotherapy. Although the clinically useful semisynthetic artemisinin derivatives are rapid acting and potent antimalarial drugs, they have short half-lives and must be administered over a period of 5-7 days, leading to noncompliance and recrudescence. With this in view, many synthetic antimalarial peroxides have been prepared. Yet, identification of orally active synthetic peroxide drug development candidates that are easily synthesized, inexpensive, and with good biopharmaceutical properties has been surprisingly difficult. In this review, we document the pitfalls and progress made in this endeavor. For each of 15 synthetic peroxide structural classes, we note highlights of the synthetic routes, product stereochemistry, and origin of the peroxide O atoms. Both in vitro and in vivo antimalarial data are then discussed and any SAR noted. Available data indicates that several synthetic 1,2,4-trioxanes are only marginally less effective than the semisynthetic artemisinins. Within a given peroxide chemical family, the more lipophilic members are more potent and possess better oral antimalarial activity in animal models than their more polar counterparts. This poses a challenge to identify peroxide structures with suitable "drug-like" physicochemical properties. Nonetheless, substantial progress has been made in the identification of a new generation of synthetic antimalarial peroxides.

show abstract

“…Recently, Robert and Meunier reviewed their mechanistic study on QHS derivatives [526,527,545,546]. They identified some adducts of heme and the primary C-centered free radical 165 through the mesoposition from the reaction of QHS with Fe(III)-heme and 2, 3-dimethylhydroquinone in methylene chloride [547] or Fe(III)-heme and glutathione in dimethyl sulfoxide [548].…”

Section: Interaction With Hemementioning

confidence: 99%

A golden phoenix arising from the herbal nest — A review and reflection on the study of antimalarial drug Qinghaosu

Liu

2010

Front. Chem. China

View full text Add to dashboard Cite

Qinghaosu (QHS) and its derivatives are a new generation of antimalarial drugs characterized by fast action, high efficacy, and good tolerance. This feature article states the discovery of QHS from traditional Chinese medicine qinghao (Artemisia annua L.) and reviews the progress during the past four decades in the research of phytochemistry of A. annua, chemical reactions and biotransformation of QHS, chemical synthesis and biosynthesis of QHS, synthesis and antimalarial activity of QHS derivatives and analogs, pharmacological studies, clinical application, and the antimalarial mechanism. Undoubtedly, QHS is an example of the value of traditional Chinese medicine in modern medicinal research.

show abstract

Recent Advances in Malaria Chemotherapy

Cited by 9 publications

References 85 publications

The State of the Art in Anti-Malarial Drug Discovery and Development

The State of the Art in Anti-Malarial Drug Discovery and Development

Synthetic peroxides as antimalarials

A golden phoenix arising from the herbal nest — A review and reflection on the study of antimalarial drug Qinghaosu

Contact Info

Product

Resources

About