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Benzothiophene derivatives as phosphodiesterase 10A (PDE10A) inhibitors: Hit-to-lead studies.

Abstract：

:A novel series of benzothiophene derivatives was discovered as phosphodiesterase 10A (PDE10A) inhibitors. Structure-activity relationship studies on high-throughput screening hit compound 1 led to the identification of 7-acetyl-3-methyl-N-(quinolin-2-yl)-1-benzothiophene-2-carboxamide (16), with potent inhibitory activity (PDE10A IC50 = 7.6 nM) and selectivity (>1300-fold selectivity over the other tested phosphodiesterases). In addition, a novel methyl-induced conformational alteration of the benzothiophene-2-carboxamide derivatives is reported.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Kawamoto Y,Tomino M,Hiramatsu K,Oyama Y,Hayashi Y

doi

10.1016/j.bmcl.2019.03.021

subject

Has Abstract

pub_date

2019-06-01 00:00:00

pages

1419-1422

issue

11

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(19)30160-X

journal_volume

29

pub_type

杂志文章

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