Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376014 | Bioorganic & Medicinal Chemistry Letters | 2005 | 4 Pages |
Abstract
Several azaline B analogs (2–10) were synthesized and evaluated for their ability to antagonize GnRH in vitro and for duration of action in inhibiting luteinizing hormone secretion in a castrated male rat assay in vivo. Analogs, 8 (IC50 = 1.85 nM), and 9 (IC50 = 1.78 nM), are equipotent with azaline B (1, IC50 = 1.36 nM) in vitro. Whereas 9 is short acting, 8 is as long acting as azaline B. Other analogs have IC50 greater than 2.0 nM and are all short acting.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Manoj P. Samant, Jozsef Gulyas, Doley J. Hong, Glenn Croston, Catherine Rivier, Jean Rivier,