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Bicyclo((aryl)methyl)benzamides as inhibitors of GlyT1.

Abstract：

:A series of isoquinuclidine benzamides as glycine uptake inhibitors for the treatment of schizophrenia are described. Potency, lipophilicity, and intrinsic human microsomal clearance were parameters for optimization. Potency correlated with the nature of the ortho substituents of the benzamide ring, and reductions in lipophilicity could be achieved through heteroatom incorporation in the benzamide and pendant phenyl moieties. Improvements in human CLint were achieved through changes in ring size and the N-alkyl group of the isoquinuclidine itself, with des-alkyl derivatives (40-41, 44) demonstrating the most robust microsomal stability. Dimethylbenzamide 9 was tested in a mouse MK801 LMA assay and had a statistically significant attenuation of locomotor activity at 3 and 10 μmol/kg compared to control.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Varnes JG,Xiong H,Forst JM,Holmquist CR,Ernst GE,Frietze W,Dembofsky B,Andisik DW,Palmer WE,Hinkley L,Steelman GB,Wilkins DE,Tian G,Jonak G,Potts WM,Wang X,Brugel TA,Alhambra C,Wood MW,Veale CA,Albert JS

doi

10.1016/j.bmcl.2018.02.029

subject

Has Abstract

pub_date

2018-04-01 00:00:00

pages

1043-1049

issue

6

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(18)30122-7

journal_volume

28

pub_type

杂志文章

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