The present invention relates to synthetic cationic lipids, liposome formulations and the use of such compounds to introduce functional bioactive agents into cultured cells.
本发明涉及合成阳离子脂质、脂质体配方以及利用这些化合物将功能性生物活性剂引入培养细胞中的用途。
Cyclisation studies of O-benzylhydroxyguanidines: synthesis of N-hydroxyimidazolines and N-hydroxypyrimidones
作者:Malcolm M. Campbell、Alexander C. Campbell、Alistair Peace、Jack Pick、Gilbert F. Woods
DOI:10.1039/c39850001164
日期:——
Two new classes of N-hydroxy heterocycles, N-hydroxy-2-imidazolines and N-hydroxypyrimidones, were synthesized by chemoselective intramolecular cyclisations.
通过化学选择性分子内环化合成了两类新的N-羟基杂环,N-羟基-2-咪唑啉和N-羟基嘧啶。
3-Alkyl-6-Chloro-2-pyrones: Selective Inhibitors of Pancreatic Cholesterol Esterase
作者:Lorraine M. Deck、Miranda L. Baca、Stephanie L. Salas、Lucy A. Hunsaker、David L. Vander Jagt
DOI:10.1021/jm990309x
日期:1999.10.1
A series of 3-alkyl-6-chloro-2-pyrones with cyclohexane rings tethered to the S-position was synthesized. The tether ranged from 0 to 4 methylene units. Inhibition of pancreatic-cholesterol esterase by this series of pyrones was markedly dependent upon the length of the tether. Dissociation constants as low as 25 nM were observed for 6-chloro-3-(1-ethyl-2-cyclohexyl)-2-pyranone. This class of cholesterol esterase inhibitors functioned as simple competitive inhibitors of substrate binding rather than as suicide substrates or active site inactivators. Trypsin and chymotrypsin were not strongly inhibited by this class of pyrones. Selectivities for cholesterol esterase were greater than 10(3). This is in contrast to 3-aryl-6-chloro-2-pyrones which are nonselective, irreversible inactivators of serine hydrolases, Thus, replacement of the 3-aryl group by an appropriately tethered 3-alkyl ring can produce highly selective inhibitors of cholesterol esterase. A second series of halogen-containing esters was prepared in which cholesterol was esterified with alpha-haloacyl halides. These haloesters were simple substrates of cholesterol esterase with no evidence of irreversible inactivation.
CAMPBELL, M. M.;CAMPBELL, A. C.;PEACE, A.;PICK, J.;WOODS, G. F., J. CHEM. SOC. CHEM. COMMUN., 1985, N 17, 1164-1165
作者:CAMPBELL, M. M.、CAMPBELL, A. C.、PEACE, A.、PICK, J.、WOODS, G. F.