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. 2019 Feb 15;11(9):2226–2242. doi: 10.1002/cctc.201801829

Scheme 11.

Scheme 11

Late‐stage diversification of human phosphodiesterase‐2 (PDE2) inhibitor 50 using liver microsomes of different animals. The analogue 51 c was observed to have a 10‐fold increased potency, an increased metabolic stability and a slightly decreased membrane permeability relative to the parent lead compound 50.156