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2-(3,5-Dimethylphenyl)tryptamine derivatives that bind to the GnRH receptor
1Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. peter_lin@merck.com
Bioorganic & Medicinal Chemistry Letters
|May 1, 2001
Abstract:
A series of 2-(3,5-dimethylphenyl)tryptamine derivatives was prepared and evaluated on a rat gonadotropin releasing hormone receptor assay. Some para-substituents on the 4-phenylbutyl side chain attached to the tryptamine nitrogen led to compounds with potent GnRH receptor binding. The study has helped define structural requirements for GnRH receptor binding for the 2-aryltryptamine GnRH antagonists.