502509-08-2Relevant articles and documents
Modification of the pyridine moiety of non-peptidyl indole GnRH receptor antagonists.
Simeone, Joseph P,Bugianesi, Robert L,Ponpipom, Mitree M,Yang, Yi Tien,Lo, Jane-Ling,Yudkovitz, Joel B,Cui, Jisong,Mount, George R,Ren, Rena Ning,Creighton, Mellissa,Mao, An-Hua,Vincent, Stella H,Cheng, Kang,Goulet, Mark T
, p. 3329 - 3332 (2007/10/03)
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.