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<atl>2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Mar2002, Vol. 12 Issue 5, p827. 6p. - Publication Year :
- 2002
-
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. [Copyright &y& Elsevier]
- Subjects :
- *GONADOTROPIN releasing hormone
*TRYPTAMINE
*HORMONE antagonists
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 12
- Issue :
- 5
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 7755961
- Full Text :
- https://doi.org/10.1016/S0960-894X(02)00026-4