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 OpenSourceMalaria (OSM
; triazolopyrazine; scaffold; OpenSourceMalaria; 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 OpenSourceMalaria (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
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Graphical Abstract
Scheme 1:
Synthesis of ether triazolopyrazine derivatives 4–9.
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 OpenSourceMalaria 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 OpenSourceMalaria 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
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Graphical Abstract
Figure 1:
Structures of some current front-line anthelmintics discussed in this review. *Denotes the stereoge...