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Synthesis of 4-(5-(2-methoxy-2-methylpropoxy)-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile #238

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alintheopen opened this issue Jul 26, 2014 · 1 comment

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@alintheopen alintheopen commented Jul 26, 2014

Following discussion (Issue #232) a selection of target compounds for the second round of biological evaluation for the triazolopyrazines.

This compound is a representative example from the chiral ethers that could be resolved by preparative HPLC at a later stage in the project. It also meets 3 of the 4 ESAC criteria:

Aim for log P between 1.5 and 3.5 (well CLogP...need to clarify)
Revisit other cores with good metabolic profiles, e.g. MMV669846
Use more sp3 carbons, and de-planarize through chirality at C-5 or in substitutions at C-2 or C-5
gh 238

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@alintheopen alintheopen commented Nov 23, 2015

Currently closing para nitrile compounds as para-difluoromethoxy compounds were preferentially targeted (http://malaria.ourexperiment.org/biological_data/11080/Results_for_samples_sent_for_in_vitro_efficacy_evaluation_against_Plasmodium_falciparum_asexual_blood_stage.html) We may revisit these compounds in relation to #304 but currently prioritising compounds here #358.

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