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What is OSM Series 4?
The Triazolopyrazine (TP) Series, or Series 4, is the latest of the OSM series. It was announced by MMV and on the OSM blog via the briefing document and as a general description on September 10th 2013.
The series arises from work performed at Pfizer (that cannot be fully disclosed) which was followed by some hit-to-lead work funded directly by MMV and performed by a CRO (which can). The series includes many potent compounds, some with promising physicochemical properties, that are non-toxic and which clear assays such as hERG. Most importantly, members of the series have proven to be potent in vivo.
Aims, Concerns and Current Interest in Series 4
Modification of Core Triazolopyrazine
Modification of Pyrazine Substitution Pattern
Modification of the Triazole Substitution
Pyrazine Side Chain Modifications - Ethers
Pyrazine Side Chain Modifications - Amides
Pyrazine Side Chain Modifications - Reversed Amides
Pyrazine Side Chain Modifications - Others
Biological Data Currently not Incorporated into the Main Wiki Sections
Mechanism of Action: Possible PfATP4 Activity Deduced from Parasite Ion Regulation Assays
Synthesis of the Ether-Linked Series
Synthesis of the Amide-Linked Series
Synthesis of the Reverse Amide- Linked Series
Synthesis of Benzylic Functionalised Ether-Linked Series
Alternative Routes to the Triazolopyrazine Core
Triazolopyrazine telesubstitution
Chirality/Stereogenic Centres in This Series
Other Sources of Compounds Relevant to this Series
Desirable Compounds Not Yet Synthesised