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Potency vs. Resistant Strains
A representative compound from the series (MMV669844 (OSM-S-218)) was evaluated against resistant strains and found to be potent, i.e. no cross-resistance was observed.
Strains examined: Dd2, Dd2 DDD107498, Dd2 FOS-R, Dd2 390048, Dd2 DSM265, Dd2 GNF156, Dd2 ELQ300, NF54, K1, 7G8, TM90C2B, Cam3.I (MRA1240)
Raw data. can also be found here. Relevant GHI.
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