|
|||||
|
|
2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain |
|
| Authors: | Young Jonathan R Huang Song X Walsh Thomas F Wyvratt Matthew J Yang Yi Tien Yudkovitz Joel B Cui Jisong Mount George R Ren Rena Ning Wu Tsuei Ju Shen Xiaolan Lyons Kathryn A Mao An Hua Carlin Josephine R Karanam Bindhu V Vincent Stella H Cheng Kang Goulet Mark T |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, NJ Rahway 07065-0900, USA. young@merck.com |
| Abstract: | A series of 2-arylindoles containing novel heteroaromatic substituents on the tryptamine tether, based on compound 1, was prepared and evaluated for their ability to act as gonadotropin releasing hormone (GnRH) antagonists. Successful modifications of 1 included chain length variation (reduction) and replacement of the pyridine with heteroaromatic groups. These alterations culminated in the discovery of compound 27kk which had excellent in vitro potency and oral efficacy in rodents. |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |