Abstract
Historically, one of the key problems in neglected disease drug discovery has been identifying new and interesting chemotypes. Phenotypic screening of the malaria parasite, Plasmodium falciparum has yielded almost 30,000 submicromolar hits in recent years. To make this collection more accessible, a collection of 400 chemotypes has been assembled, termed the Malaria Box. Half of these compounds were selected based on their drug-like properties and the others as molecular probes. These can now be requested as a pharmacological test set by malaria biologists, but importantly by groups working on related parasites, as part of a program to make both data and compounds readily available. In this paper, the analysis and selection methodology and characteristics of the compounds are described.
Highlights
260 million people are affected each year by malaria, with around 655,000 deaths
A dispersible fixed dose combination of artemether and lumefantrine designed for children, CoartemH-Dispersible was developed by a collaboration of Medicines for Malaria Venture (MMV) [Medicines for Malaria Venture (MMV) is a not for profit public private partnership whose focus is on the discovery, development and launch of small molecule anti-malarial agents
Chemical diversity of the dataset Given the limitations on the number of compounds that can be tested in detail, to maximize the potential impact of the Malaria Box it was important to maximize the structural diversity in the compounds selected [16]
Summary
260 million people are affected each year by malaria, with around 655,000 deaths. The current gold standard treatments for malaria are the artemisinin combination therapies: combinations of derivatives of the natural product artemisinin, and aminoquinolines or aminoalcohols, the descendants of quinine [2,3,4] Five such artemisinin combination therapies have been approved by either stringent regulatory authorities or the World Health Organization’s prequalification department. There is continually concern that P. falciparum strains with decreased speed of parasite killing are present in the border regions of Cambodia, Thailand and Myanmar [5,6]. This is putting increased pressure on the partner medication, and highlighting an urgent need for the development of new anti-malarial medicines over the decade [1],[4]. To further support the malaria eradication agenda new drugs with transmission blocking or liver stage activity are required [7,8,9,10]
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