Bioorganic & medicinal chemistry letters, 2010-02, Vol.20 (3), p.881-886
- Tice, Colin M.
- Zhao, Wei
- Xu, Zhenrong
- Cacatian, Salvacion T.
- Simpson, Robert D.
- Ye, Yuan-Jie
- Singh, Suresh B.
- McKeever, Brian M.
- Lindblom, Peter
- Guo, Joan
- Krosky, Paula M.
- Kruk, Barbara A.
- Berbaum, Jennifer
- Harrison, Richard K.
- Johnson, Judith J.
- Bukhtiyarov, Yuri
- Panemangalore, Reshma
- Scott, Boyd B.
- Zhao, Yi
- Bruno, Joseph G.
- Zhuang, Linghang
- McGeehan, Gerard M.
- He, Wei
- Claremon, David A.
2010
Volltextzugriff (PDF)
Details
- Autor(en) / Beteiligte
- Tice, Colin M.
- Zhao, Wei
- Xu, Zhenrong
- Cacatian, Salvacion T.
- Simpson, Robert D.
- Ye, Yuan-Jie
- Singh, Suresh B.
- McKeever, Brian M.
- Lindblom, Peter
- Guo, Joan
- Krosky, Paula M.
- Kruk, Barbara A.
- Berbaum, Jennifer
- Harrison, Richard K.
- Johnson, Judith J.
- Bukhtiyarov, Yuri
- Panemangalore, Reshma
- Scott, Boyd B.
- Zhao, Yi
- Bruno, Joseph G.
- Zhuang, Linghang
- McGeehan, Gerard M.
- He, Wei
- Claremon, David A.
- Titel
- Spirocyclic ureas: Orally bioavailable 11β-HSD1 inhibitors identified by computer-aided drug design
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2010-02, Vol.20 (3), p.881-886
- Ort / Verlag
- England: Elsevier Ltd
- Erscheinungsjahr
- 2010
- Quelle
- Access via ScienceDirect (Elsevier)
- Beschreibungen/Notizen
- Structure-guided drug design led to the identification of a class of spirocyclic ureas which potently inhibit human 11β-HSD1 in vitro. Lead compound 10j was shown to be orally bioavailable in three species, distributed into adipose tissue in the mouse, and its (R) isomer 10j2 was efficacious in a primate pharmacodynamic model.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2009.12.082Titel-ID: cdi_proquest_miscellaneous_734276864
- Format
- –
- Schlagworte
- 11-beta-Hydroxysteroid Dehydrogenase Type 1 - antagonists & inhibitors, 11-beta-Hydroxysteroid Dehydrogenase Type 1 - metabolism, 11β-Hydroxysteroid dehydrogenase, Administration, Oral, Animals, Binding Sites - physiology, Biological Availability, CHO Cells, Cricetinae, Cricetulus, Diabetes, Drug Design, Humans, Macaca fascicularis, Mice, Rats, Spirocycles, Structure-Activity Relationship, Structure-based drug design, Urea - administration & dosage, Urea - analogs & derivatives, Urea - pharmacokinetics