1,4-Diazepane compounds as potent and selective CB2 agonists: Optimization of metabolic stability

A high-throughput screening campaign has identified 1,4-diazepane compounds which are potent Cannabinoid receptor 2 agonists with excellent selectivity against the Cannabinoid receptor 1. This class of compounds suffered from low metabolic stability. Following various strategies, compounds with a go...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-04, Vol.21 (7), p.2011-2016
Hauptverfasser:	Riether, Doris, Wu, Lifen, Cirillo, Pier F., Berry, Angela, Walker, Edward R., Ermann, Monika, Noya-Marino, Beatriz, Jenkins, James E., Albaugh, Dan, Albrecht, Claudia, Fisher, Michael, Gemkow, Mark J., Grbic, Heather, Löbbe, Sabine, Möller, Clemens, O’Shea, Kathy, Sauer, Achim, Shih, Daw-Tsun, Thomson, David S.
Format:	Artikel
Sprache:	eng
Schlagworte:	1,4-Diazepane agonists Animals Azepines - chemistry Azepines - pharmacology Biological and medical sciences Cannabinoid receptor cannabinoids CB2 liver microsomes Medical sciences Metabolic stability Microsomes, Liver - metabolism Miscellaneous Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Rats Rats, Wistar Receptor, Cannabinoid, CB2 - agonists receptors screening
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Zusammenfassung:	A high-throughput screening campaign has identified 1,4-diazepane compounds which are potent Cannabinoid receptor 2 agonists with excellent selectivity against the Cannabinoid receptor 1. This class of compounds suffered from low metabolic stability. Following various strategies, compounds with a good stability in liver microsomes and rat PK profile have been identified.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.02.017