Design and synthesis of boronic acid inhibitors of endothelial lipase
Endothelial lipase (EL) and lipoprotein lipase (LPL) are homologous lipases that act on plasma lipoproteins. EL is predominantly a phospholipase and appears to be a key regulator of plasma HDL-C. LPL is mainly a triglyceride lipase regulating (V)LDL levels. The existing biological data indicate that inhibitors selective for EL over LPL should have anti-atherogenic activity, mainly through increasing plasma HDL-C levels. We report here the synthesis of alkyl, aryl, or acyl-substituted phenylboronic acids that inhibit EL. Many of the inhibitors evaluated proved to be nearly equally potent against both EL and LPL, but several exhibited moderate to good selectivity for EL.
O'Connell, Daniel P.,Leblanc, Daniel F.,Cromley, Debra,Billheimer, Jeffrey,Rader, Daniel J.,Bachovchin, William W.
p. 1397 - 1401
(2012/03/26)
BI-ARYL COMPOUND HAVING IMMUNOSUPPRESSIVE ACTIVITY
The invention is directed to a bi-aryl compound having a unique immunomodulating activity, a process for a preparation thereof, a pharmaceutical composition containing the same, and a method of preventing or treating disorders or diseases mediated by T lymphocytes by administering the compound to a subject in need of treatment.
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Page/Page column 46; 47
(2010/02/10)
Highly efficient syntheses of 3-aryl-2-cycloalken-1-ones and an evaluation of their liquid crystalline properties
Cycloalkenones are shown to be mesogens and can be synthesised in near quantitative yields by a convergent palladium(0)-catalysed cross-coupling strategy; a 2-methyl group induces a change of phase from smectic to nematic.
Marson,Farrand,Brettle,Dunmur
p. 4377 - 4381
(2007/10/03)
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