910789-99-0Relevant academic research and scientific papers
Discovery of orally active butyrolactam 11β-HSD1 inhibitors
Yeh, Vince S.C.,Kurukulasuriya, Ravi,Fung, Steven,Monzon, Katina,Chiou, William,Wang, Jiahong,Stolarik, Deanne,Imade, Hovis,Shapiro, Robin,Knourek-Segel, Victoria,Bush, Eugene,Wilcox, Denise,Nguyen, Phong T.,Brune, Michael,Jacobson, Peer,Link
, p. 5555 - 5560 (2007/10/03)
A series of metabolically stable butyrolactam 11β-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity, pharmacokinetic, and pharmacodynamic profiles.
A highly efficient synthesis of potent and selective butyrolactam inhibitors of 11β-Hsd1
Yeh, Vince S. C.,Kurukulasuriya, Ravi,Kerdesky, Francis A.
, p. 3963 - 3966 (2007/10/03)
A convergent synthesis of structurally novel butyrolactam 11β-HSD1 inhibitors is described. The approach features an efficient Ireland-Claisen reaction to construct a highly substituted aldehyde building block which is converted to a lactam via a tandem r
