-
Notifications
You must be signed in to change notification settings - Fork 3
Gametocyte Stage
The original Series 4 briefing document stated the series had "no or weak >>1uM activity against gametocytes" but there are no associated data to support this statement.
As was discussed, a mechanism of action vs. PfATP4 is compatible with activity vs. gametocytes. Representative series members were collected for analysis in a relevant assay and the resulting data showed that weak activity vs male gamete formation was observed.
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