Synthesis, in vivo and in vitro biological activity of novel azaline B analogs

[Display omitted] 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 (IC 50 = 1.85 nM), and 9 (IC 50 = 1.78 nM), are e...

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Published in:Bioorganic & medicinal chemistry letters 2005-06, Vol.15 (11), p.2894-2897
Main Authors: Samant, Manoj P., Gulyas, Jozsef, Hong, Doley J., Croston, Glenn, Rivier, Catherine, Rivier, Jean
Format: Article
Language:English
Subjects:
Animals
Azaline B
Biological and medical sciences
Cell Line
Chromatography, High Pressure Liquid
Degarelix
GnRH antagonists
Gonadotropin-Releasing Hormone - analogs & derivatives
Gonadotropin-Releasing Hormone - antagonists & inhibitors
Gonadotropin-Releasing Hormone - chemical synthesis
Gonadotropin-Releasing Hormone - chemistry
Gonadotropin-Releasing Hormone - pharmacology
Hormones. Endocrine system
Humans
Male
Medical sciences
Pharmacology. Drug treatments
Rats
Structure activity relationships
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Summary:[Display omitted] 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 (IC 50 = 1.85 nM), and 9 (IC 50 = 1.78 nM), are equipotent with azaline B ( 1, IC 50 = 1.36 nM) in vitro. Whereas 9 is short acting, 8 is as long acting as azaline B. Other analogs have IC 50 greater than 2.0 nM and are all short acting.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.03.085