Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1).

High-throughput screening of a small-molecule compound library resulted in the identification of a series of arylsulfonylpiperazines that are potent and selective inhibitors of human 11beta-Hydroxysteroid Dehydrogenase Type 1 (11beta-HSD1). Optimization of the initial lead resulted in the discovery of compound (R)-45 (11beta-HSD1 IC(50)=3nM).

Infrared spectroscopic investigations on the metallation of terminal alkynes by Zn(OTf)2.

An IR study of terminal acetylenes and Zn(OTf)(2) in the presence of amine bases provides evidence that is consistent with the generation of Zn-acetylides.