Zwitterionic Sulfobetaine Inhibitors of Squalene Synthase
作者:Thomas A. Spencer、Thomas J. Onofrey、Reginald O. Cann、Jonathon S. Russel、Laura E. Lee、Daniel E. Blanchard、Alfredo Castro、Peide Gu、Guojian Jiang、Ishaiahu Shechter
DOI:10.1021/jo981617q
日期:1999.2.1
A substantial number of sulfobetaines (e.g., 10) have been synthesized and evaluated as inhibitors of squalenesynthase (SS) on the basis of the idea that their zwitterionic structure would have properties conducive both to binding in the active site and to passage through cell membranes. When the simple sulfobetaine moiety is incorporated into compounds containing hydrophobic portions like those in
Enantioselective Remote C(sp<sup>3</sup>)–H Cyanation via Dual Photoredox and Copper Catalysis
作者:Hui Chen、Weiwei Jin、Shouyun Yu
DOI:10.1021/acs.orglett.0c02008
日期:2020.8.7
The remote C(sp3)–H cyanation of carboxamides has been described by merging photoredox and copper catalysis in a site-selective and enantiocontrolled manner. The protocol is the integration of photoinduced and nitrogen-centered radical-mediated intermolecular hydrogen atom transfer with chiral copper-complex-catalyzed radical cyanation. This strategy gives enantio-enriched cyanated amides in high yields
Assay and inhibition of diacylglycerol lipase activity
作者:Meghan Johnston、Shachi R. Bhatt、Surina Sikka、Richard W. Mercier、Jay M. West、Alexandros Makriyannis、S. John Gatley、Richard I. Duclos
DOI:10.1016/j.bmcl.2012.05.101
日期:2012.7
acid esters of β-lactone derivatives structurally related to tetrahydrolipstatin (THL) and O-3841 were synthesized that inhibit human and murine diacylglycerol lipase (DAGL) activities. New ether lipid reporter compounds were developed for an in vitro assay to efficiently screen inhibitors of 1,2-diacyl-sn-glycerol hydrolysis and related lipase activities using fluorescence resonance energy transfer (FRET)