当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis and biological evaluation of 3-biphenyl-4-yl-4-phenyl-4H-1,2,4-triazoles as novel glycine transporter 1 inhibitors.

Synthesis and biological evaluation of 3-biphenyl-4-yl-4-phenyl-4H-1,2,4-triazoles as novel glycine transporter 1 inhibitors.

Abstract：

:We describe the preparation and evaluation of a novel series of glycine transporter 1 (GlyT1) inhibitors derived from a high-throughput screening hit. The SAR studies resulted in the discovery of 3-biphenyl-4-yl-4-(2-fluorophenyl)-5-isopropyl-4H-1,2,4-triazole (6p). A pharmacokinetic study was also conducted and revealed that 6p had excellent oral bioavailability and ameliorated learning impairment in passive avoidance tasks in mice.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Sugane T,Tobe T,Hamaguchi W,Shimada I,Maeno K,Miyata J,Suzuki T,Kimizuka T,Kohara A,Morita T,Doihara H,Saita K,Aota M,Furutani M,Shimada Y,Hamada N,Sakamoto S,Tsukamoto S

doi

10.1021/jm101031u

subject

Has Abstract

pub_date

2011-01-13 00:00:00

pages

387-91

issue

1

eissn

0022-2623

issn

1520-4804

journal_volume

54

pub_type

杂志文章

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