Synthesis and biological evaluation of alpha-sulfonamido-N-adamantanecarboxamide derivatives as 11 beta-HSD1 inhibitors

Young Hoon Kim,Seung Kyu Kang, Gwi Bin Lee,Kyu Myung Lee,Jaladi Ashok Kumar,Ki Young Kim,Sang Dal Rhee, Jeongmin Joo,Myung Ae Bae,Won Koo Lee,Jin Hee Ahn

MedChemComm（2015）

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摘要

A series of alpha-sulfonamido-N-adamantanecarboxamide derivatives as 11 beta-HSD1 inhibitors was identified. Among them, compound 7j was the most active with an IC50 value of 8 nM in humans 11 beta-HSD1. Compound 7j exhibited reasonable stability, permeability and safety profiles (CYP and hERG). Compound 7j showed good ex vivo 11 beta-HSD1 inhibition with similar to 80% inhibition after 20 MPK oral dosing.

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