An article about strategy for extending half life in vivo

In compound optimization stage, “reduce lipophilicity” is mantra for chemists. High lipophilicity compound tend to be metabolically unstable, promiscuous and binding many off targets. To reduce lipophilicity is important strategy for drug discovery process but it is not always suitable strategy. Researchers from Genentech report their useful experience in JMC lett. You can find theContinue reading “An article about strategy for extending half life in vivo”

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An article about PDE2a Inhibitors

I read an article on my way to work in this morning. It was very exciting article for me. A story about PDE2a inhibitors. http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.6b01793 PDE2a is one of Phosphodiesterase family and be interested in PDE inhibitors for the treatment of CNS disorders. In the article, the SAR started from HTS hit 3. They gotContinue reading “An article about PDE2a Inhibitors”