当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > The discovery and characterization of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor potentiator N-{(3S,4S)-4-[4-(5-cyano-2-thienyl)phenoxy]tetrahydrofuran-3-yl}propane-2-sulfonamide (PF-04958242).

The discovery and characterization of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor potentiator N-{(3S,4S)-4-[4-(5-cyano-2-thienyl)phenoxy]tetrahydrofuran-3-yl}propane-2-sulfonamide (PF-04958242).

Abstract：

:A unique tetrahydrofuran ether class of highly potent α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor potentiators has been identified using rational and structure-based drug design. An acyclic lead compound, containing an ether-linked isopropylsulfonamide and biphenyl group, was pharmacologically augmented by converting it to a conformationally constrained tetrahydrofuran to improve key interactions with the human GluA2 ligand-binding domain. Subsequent replacement of the distal phenyl motif with 2-cyanothiophene to enhance its potency, selectivity, and metabolic stability afforded N-{(3S,4S)-4-[4-(5-cyano-2-thienyl)phenoxy]tetrahydrofuran-3-yl}propane-2-sulfonamide (PF-04958242, 3), whose preclinical characterization suggests an adequate therapeutic index, aided by low projected human oral pharmacokinetic variability, for clinical studies exploring its ability to attenuate cognitive deficits in patients with schizophrenia.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Shaffer CL,Patel NC,Schwarz J,Scialis RJ,Wei Y,Hou XJ,Xie L,Karki K,Bryce DK,Osgood SM,Hoffmann WE,Lazzaro JT,Chang C,McGinnis DF,Lotarski SM,Liu J,Obach RS,Weber ML,Chen L,Zasadny KR,Seymour PA,Schmidt CJ,Haj

doi

10.1021/acs.jmedchem.5b00300

subject

Has Abstract

pub_date

2015-05-28 00:00:00

pages

4291-308

issue

10

eissn

0022-2623

issn

1520-4804

journal_volume

58

pub_type

杂志文章

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