Skip to content
New issue

Have a question about this project? Sign up for a free GitHub account to open an issue and contact its maintainers and the community.

By clicking “Sign up for GitHub”, you agree to our terms of service and privacy statement. We’ll occasionally send you account related emails.

Already on GitHub? Sign in to your account

Synthesis of 4-(5-(2-methoxypropoxy)-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile #239

Closed
alintheopen opened this issue Jul 26, 2014 · 1 comment

Comments

@alintheopen
Copy link
Member

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 239

@alintheopen
Copy link
Member Author

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.

Sign up for free to join this conversation on GitHub. Already have an account? Sign in to comment
Projects
None yet
Development

No branches or pull requests

1 participant