| Literature DB >> 18485702 |
Haixia Wang1, Zheming Ruan, James J Li, Ligaya M Simpkins, Rebecca A Smirk, Shung C Wu, Robert D Hutchins, David S Nirschl, Katy Van Kirk, Christopher B Cooper, James C Sutton, Zhengping Ma, Rajasree Golla, Ramakrishna Seethala, Mary Ellen K Salyan, Akbar Nayeem, Stanley R Krystek, Steven Sheriff, Daniel M Camac, Paul E Morin, Brian Carpenter, Jeffrey A Robl, Robert Zahler, David A Gordon, Lawrence G Hamann.
Abstract
Several series of pyridine amides were identified as selective and potent 11beta-HSD1 inhibitors. The most potent inhibitors feature 2,6- or 3,5-disubstitution on the pyridine core. Various linkers (CH(2)SO(2), CH(2)S, CH(2)O, 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 11beta-HSD1 and the most potent inhibitor in this series.Entities:
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Year: 2008 PMID： 18485702 DOI： 10.1016/j.bmcl.2008.04.069
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823