Issue 7, 2015

Synthesis and biological evaluation of α-sulfonamido-N-adamantanecarboxamide derivatives as 11β-HSD1 inhibitors

Abstract

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

Graphical abstract: Synthesis and biological evaluation of α-sulfonamido-N-adamantanecarboxamide derivatives as 11β-HSD1 inhibitors

Article information

Article type
Concise Article
Submitted
08 Mar 2015
Accepted
25 May 2015
First published
17 Jun 2015

Med. Chem. Commun., 2015,6, 1360-1369

Author version available

Synthesis and biological evaluation of α-sulfonamido-N-adamantanecarboxamide derivatives as 11β-HSD1 inhibitors

Y. H. Kim, S. K. Kang, G. B. Lee, K. M. Lee, J. A. Kumar, K. Y. Kim, S. D. Rhee, J. Joo, M. A. Bae, W. K. Lee and J. H. Ahn, Med. Chem. Commun., 2015, 6, 1360 DOI: 10.1039/C5MD00096C

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