Title of article
Pyridine amides as potent and selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1
Author/Authors
Haixia Wang، نويسنده , , Zheming Ruan، نويسنده , , James J. Li، نويسنده , , Ligaya M. Simpkins، نويسنده , , Rebecca A. Smirk، نويسنده , , Shung C. Wu، نويسنده , , Robert D. Hutchins، نويسنده , , David S. Nirschl، نويسنده , , Katy Van Kirk، نويسنده , , Christopher B. Cooper، نويسنده , , James C. Sutton، نويسنده , , Zhengping Ma، نويسنده , , Rajasree Golla، نويسنده , , Ramakrishna Seethala، نويسنده , , Mary Ellen K. Salyan، نويسنده , , Akbar Nayeem، نويسنده , , Stanley R. Krystek Jr.، نويسنده , , Steven Sheriff، نويسنده , , Daniel M. Camac، نويسنده , , Paul E. Morin، نويسنده , , et al.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
3168
To page
3172
Abstract
Several series of pyridine amides were identified as selective and potent 11β-HSD1 inhibitors. The most potent inhibitors feature 2,6- or 3,5-disubstitution on the pyridine core. Various linkers (CH2SO2, CH2S, CH2O, S, O, N, bond) between the distal aryl and central pyridyl groups are tolerated, and lipophilic amide groups are generally favored. On the distal aryl group, a number of substitutions are well tolerated. A crystal structure was obtained for a complex between 11β-HSD1 and the most potent inhibitor in this series.
Keywords
Pyridine amide , 11?-Hydroxysteroid dehydrogenase type 1 , 11?-HSD1
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799523
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