In 2012, there were an estimated 207 million cases of malaria and over 600 thousand deaths.1 Frontline treatments for malaria are currently artemisin combination therapies (ACTs). However, the inevitable reports of resistance or tolerance have already appeared and so new medicines that can replace and complement the ACTs for blood stage falciparum malaria are urgently needed. The Open Source Malaria (OSM)2 project involves a hit-to-lead campaign in antimalarial drug discovery. The project was initiated with the synthesis of some known active compounds from the GlaxoSmithKline open dataset.3 Once the activities were confirmed, OSM chemists began synthesis and evaluation of four series of compounds; aryl pyrroles, ‘near-neighbours’, aminothienopyrimidines and triazolopyrazines. Open source drug discovery operates on the principles that all data and ideas should be freely shared, anyone may participate at any level and there will be no patents.4 By working in this manner, research is accelerated through the recruitment of expertise from a variety of participants. Synthetic chemistry and biological evaluations are recorded using online electronic laboratory notebooks.5 Project coordination is effected through the use of online project management tools, and participants are encouraged to join the project through social media. The open nature of the project means that anyone can take part and this has led to wide ranging contributions from a truly international and interdisciplinary team. Thus the iterative cycle of analog synthesis in response to biological data that is normally guided by luck and medchem intuition is now guided by the intuition of the collective. 1WHO World Malaria Report 2013 (http://www.who.int/malaria/publications/world_malaria_report_2013/report/en/); 2opensourcemalaria.org and @O_S_M; 3Nature 2010, 465, 305–310; 4Parasitology 2014, 141, 148–157; 5Chem. Sci. 2014, DOI: 10.1039/C4SC02128B.

Open source malaria: A new approach to drug discovery

249th National Meeting (2015)

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