Literature DB >> 12392744

Modification of the pyridine moiety of non-peptidyl indole GnRH receptor antagonists.

Joseph P Simeone1, Robert L Bugianesi, Mitree M Ponpipom, Yi Tien Yang, Jane-Ling Lo, Joel B Yudkovitz, Jisong Cui, George R Mount, Rena Ning Ren, Mellissa Creighton, An-Hua Mao, Stella H Vincent, Kang Cheng, Mark T Goulet.   

Abstract

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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Year:  2002        PMID: 12392744     DOI: 10.1016/s0960-894x(02)00751-5

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

Review 1.  Recent Development of Non-Peptide GnRH Antagonists.

Authors:  Feng-Ling Tukun; Dag Erlend Olberg; Patrick J Riss; Ira Haraldsen; Anita Kaass; Jo Klaveness
Journal:  Molecules       Date:  2017-12-09       Impact factor: 4.411

  1 in total

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