Bioorganic and Medicinal Chemistry Letters p. 5599 - 5603 (2004)
Update date:2022-08-03
Topics:
DeVita, Robert J.
Parikh, Mamta
Jiang, Jinlong
Fair, Jason A.
Young, Jonathan R.
Walsh, Thomas F.
Goulet, Mark T.
Lo, Jane-L.
Ren, Ning
Yudkovitz, Joel B.
Cui, Jisong
Yang, Yi T.
Cheng, Kang
Rohrer, Susan P.
Wyvratt, Matthew J.
Potent neutral replacements of the basic amine at the 4-position of quinolone non-peptide GnRH antagonists are reported. A series of neutral, nonbasic quinolone GnRH antagonists were prepared via Mitsunobu alkylation of protected and unprotected 4-hydroxy quinolone intermediates. The synthetic route was improved by utilization of unique reactivity and convergency afforded by the use of mono and bis-trimethylsilylethyl protected quinolones. Potent neutral GnRH antagonists were identified, including ether and lactam derivatives, that show similar in vitro binding affinity and functional activity as compared to the earlier basic 4-aminoalkyl quinolone series of nonpeptide GnRH antagonists.
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