Bioorganic and Medicinal Chemistry Letters p. 2597 - 2602 (2001)
Update date:2022-08-05
Topics: Oral Bioavailability Nonpeptide
Ashton, Wallace T.
Sisco, Rosemary M.
Kieczykowski, Gerard R.
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.
Stereospecific introduction of a methyl group to the indole-3-side chain enhanced activity in our tryptamine-derived series of GnRH receptor antagonists. Further improvements were achieved by variation of the bicyclic amino moiety of the tertiary amide and by adjustment of the tether length to a pyridine or pyridone terminus. These modifications culminated in analogue 24, which had oral activity in a rat model and acceptable oral bioavailability and half-life in dogs and monkeys.
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