Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation |
| |
| Authors: | Patel Jyoti R Shuai Qi Dinges Jurgen Winn Marty Pliushchev Marina Fung Steven Monzon Katina Chiou William Wang Jiahong Pan Liping Wagaw Seble Engstrom Kenneth Kerdesky Francis A Longenecker Kenton Judge Russell Qin Wenying Imade Hovis M Stolarik Deanne Beno David W A Brune Michael Chovan Linda E Sham Hing L Jacobson Peer Link J T |
| |
| Institution: | Global Pharmaceutical Research & Development, Abbott Laboratories, R43G, AP52, 200 Abbott Park Road, Abbott Park, IL-60064-6217, USA. jyoti.patel@abbott.com |
| |
| Abstract: | A novel class of adamantane ethers 11beta-hydroxysteroid hydrogenase type I inhibitors has been discovered. These compounds have excellent HSD-1 potency and selectivity against HSD-2. The structure-activity relationships, selectivity, metabolism, PK, ex vivo pharmacodynamic data, and an X-ray crystal structure of one of these inhibitors bound to h-HSD-1 are discussed. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ |
|
