| Literature DB >> 11551758 |
W T Ashton1, R M Sisco, G R Kieczykowski, Y T Yang, J B Yudkovitz, J Cui, G R Mount, R N Ren, T J Wu, X Shen, K A Lyons, A H Mao, J R Carlin, B V Karanam, S H Vincent, K Cheng, M T Goulet.
Abstract
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.Entities:
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Year: 2001 PMID： 11551758 DOI： 10.1016/s0960-894x(01)00512-1
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823