Investigations of amination reactions on an antimalarial 1,2,4-triazolo[4,3-a]pyrazine scaffold

• Henry S. T. Smith,
• Ben Giuliani,
• Kanchana Wijesekera,
• Kah Yean Lum,
• Sandra Duffy,
• Aaron Lock,
• Jonathan M. White,
• Vicky M. Avery and
• Rohan A. Davis

Beilstein J. Org. Chem. 2025, 21, 1126–1134, doi:10.3762/bjoc.21.90

• School of Chemistry and Bio21 Institute, The University of Melbourne, Melbourne, VIC 3010, Australia, NatureBank, Griffith University, Brisbane, QLD 4111, Australia 10.3762/bjoc.21.90 Abstract 1,2,4-Triazolo[4,3-a]pyrazines have previously been explored by the Open Source Malaria project as potent in

• substitution; antimalarial; open source malaria; triazolopyrazine; 1,2,4-triazolo[4,3-a]pyrazines; Introduction Malarial disease is a potentially fatal, acute febrile illness caused by infection with any of several species of vector-borne apicomplexan parasites in the genus Plasmodium [1]. The African endemic

• resistant parasites [1]. Open Source Malaria (OSM) is a drug development and medicinal chemistry platform established by Matthew Todd formerly of The University of Sydney (currently at University College London) with funding from the product development partnership platform, Medicines for Malaria Venture

Synthesis and characterisation of new antimalarial fluorinated triazolopyrazine compounds

• Kah Yean Lum,
• Jonathan M. White,
• Daniel J. G. Johnson,
• Vicky M. Avery and
• Rohan A. Davis

Beilstein J. Org. Chem. 2023, 19, 107–114, doi:10.3762/bjoc.19.11

• , Australia Discovery Biology, Griffith University, Nathan, QLD 4111, Australia NatureBank, Griffith University, Nathan, QLD 4111, Australia 10.3762/bjoc.19.11 Abstract Nine new fluorinated analogues were synthesised by late-stage functionalisation using Diversinate™ chemistry on the Open Source Malaria (OSM

• ; triazolopyrazine; scaffold; Open Source Malaria; Introduction Malaria is an infectious disease caused by Plasmodium parasites and is a major global threat to human health. The WHO World Malaria Report 2021, estimates 241 million cases of malaria and 627,000 deaths globally in 2020, an increase of 12% from the

• targets are urgently needed to combat the global problem of parasite drug resistance. For more than 10 years, the Open Source Malaria (OSM) consortium [4] has had an interest in identifying and developing novel antimalarial compounds that belong to a variety of chemotypes, one of which includes the 1,2,4

Anthelmintic drug discovery: target identification, screening methods and the role of open science

• Frederick A. Partridge,
• Ruth Forman,
• Carole J. R. Bataille,
• Graham M. Wynne,
• Marina Nick,
• Angela J. Russell,
• Kathryn J. Else and
• David B. Sattelle

Beilstein J. Org. Chem. 2020, 16, 1203–1224, doi:10.3762/bjoc.16.105

• effective new drugs [79]. The latter is an open database for researchers to upload scientific data, including biological results, so that others may use it [80]. Perhaps the biggest example of open source drug discovery in its pure form is the Open Source Malaria project [81][82]. This is a platform for

• on the Github issues page of the project. Importantly, anyone is free to jump in with suggestions, and indeed the Open Source Malaria Project has been successful at receiving high-quality contributions, from a wide range of sources. A highlight of this work has been the detailed exploration of an