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Lipophilicity & lipophilic efficiency:
Few compounds achieve a lipophilic efficiency (as measured by pIC50 – AlogP) of greater than 4.0
What is OSM Series 4?
Aims, Concerns and Current Interest in Series 4
Sources of Data
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
Metabolites
Biological Data Currently not Incorporated into the Main Wiki Sections
Physicochem/metabolism/PK
Metabolism ID
Aldehyde Oxidase Assay
Liver Stage
Gametocyte Stage
In Vivo Efficacy
Potency vs. Resistant Strains
Other Observations
Mechanism of Action: Possible PfATP4 Activity Deduced from Parasite Ion Regulation Assays
hERG Activity
Toxicity
Synthetic Design
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
Biofunctionalisation
Late Stage Functionalisation
Fluoroalkene Isostere
Spectroscopy
Chirality/Stereogenic Centres in This Series
Other Sources of Compounds Relevant to this Series
Desirable Compounds Not Yet Synthesised
Evaluations vs Other Organisms
Strings for Google
