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Enhanced potency of perfluorinated thalidomide derivatives for inhibition of LPS-induced tumor necrosis factor-alpha production is associated with a change of mechanism of action.

Abstract：

:Perfluorination of phthalimides leads to dramatically increased potency as inhibitors of TNF-alpha production. We examined the enantiodependence for several tetrafluorophthalimides and alpha-methylthalidomide, 3. Only 3 exhibited strikingly enantiodependent activity. The key structural determinant for the enhanced activity is the tetrafluorophthaloyl group, which confers enhanced potency and a change in the mechanism of inhibition.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Niwayama S,Loh C,Turk BE,Liu JO,Miyachi H,Hashimoto Y

doi

10.1016/s0960-894x(98)00171-1

subject

Has Abstract

pub_date

1998-05-05 00:00:00

pages

1071-6

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960894X98001711

journal_volume

8

pub_type

杂志文章

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