The synthesis of a number of indole GnRH antagonists is described. Oxidation of the pyridine ring nitrogen, combined with alkylation at the two position, led to a compound with an excellent in vitro activity profile as well as oral bioavailability in both rats and dogs.
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| http://dx.doi.org/10.1016/s0960-894x(02)00751-5 | DOI Listing |
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