Discovery of orally active butyrolactam 11β-HSD1 inhibitors

Autor:	Jiahong Wang, DeAnne Stolarik, Hovis M. Imade, Victoria Knourek-Segel, Phong Nguyen, Denise Wilcox, Peer B. Jacobson, Michael E. Brune, William Chiou, Steven Fung, Robin Shapiro, Vince Yeh, J.T. Link, Ravi Kurukulasuriya, Katina Monzon, Eugene N. Bush
Rok vydání:	2006
Předmět:	Lactams Stereochemistry Clinical Biochemistry Administration Oral Pharmaceutical Science Biochemistry Chemical synthesis Mice chemistry.chemical_compound Oral administration In vivo 11-beta-Hydroxysteroid Dehydrogenase Type 1 Drug Discovery Animals Humans Potency Molecular Biology Metabolic Syndrome chemistry.chemical_classification biology Chemistry Organic Chemistry Enzyme Enzyme inhibitor Lactam biology.protein Molecular Medicine Selectivity hormones hormone substitutes and hormone antagonists
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 16:5555-5560
ISSN:	0960-894X
Popis:	A series of metabolically stable butyrolactam 11beta-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity, pharmacokinetic, and pharmacodynamic profiles.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16d60418fa06ac90a6a4054cde3829be https://doi.org/10.1016/j.bmcl.2006.08.034 Zobrazit plný text záznamu Full Text from ScienceDirect