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Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: hit-to-lead optimization.

Abstract：

:An HTS campaign of our corporate compound library resulted in thieno[2,3-b]pyridines derivative hits with mGluR5 negative allosteric modulator effects. During the hit-to-lead development our objective was to improve affinity, and to keep the ligand efficiency values at an acceptable level. After different modifications of the linker resulted in a 2-sulfonyl-thieno[2,3-b]pyridines derivative, which fulfilled the lead criteria.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Nógrádi K,Wágner G,Domány G,Bobok A,Magdó I,Kiss B,Kolok S,Fónagy K,Gyertyán I,Háda V,Kóti J,Gál K,Farkas S,Keserű GM,Greiner I,Szombathelyi Z

doi

10.1016/j.bmcl.2014.06.057

subject

Has Abstract

pub_date

2014-08-15 00:00:00

pages

3845-9

issue

16

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)00685-4

journal_volume

24

pub_type

杂志文章

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