Substituted indole-5-carboxamides and -acetamides as potent nonpeptide GnRH receptor antagonists. |
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| Authors: | W T Ashton R M Sisco Y T Yang J L Lo J B Yudkovitz K Cheng M T Goulet |
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| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, 07065-0900, Rahway, NJ, USA. wally_ashton@merck.com |
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| Abstract: | The 2-aryltryptamine class of GnRH receptor antagonists has been modified to incorporate carboxamide and acetamide substituents at the indole 5-position. With either a phenol or methanesulfonamide terminus on the N-aralkyl side chain, potent binding affinity to the GnRH receptor was achieved. A functional assay for GnRH antagonism was even more sensitive to structural modification and revealed a strong preference for branched tertiary amides. |
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