808172-32-9Relevant academic research and scientific papers
Identification of neutral 4-O-alkyl quinolone nonpeptide GnRH receptor antagonists
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.
, p. 5599 - 5603 (2007/10/03)
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.
