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Synthetic Design
The approach to the synthesis of Series 4 up has mainly involved the functionalization of a pyrazine core, followed by a cyclization reaction to give the triazolopyrazine which may then be subsequently functionalized. The two main series, ether- and amide-linked compounds are shown below along with a specific example of a potent compound in each series.
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