Synthesis and biological evaluation of (4H-1,2,4-triazol-4-yl)isoquinoline derivatives as selective glycine transporter 1 inhibitors.

Takashi Sugane,Takahiko Tobe,Wataru Hamaguchi,Itsuro Shimada,Kyoichi Maeno,Junji Miyata,Takeshi Suzuki,Tetsuya Kimizuka,Takuma Morita,Shuichi Sakamoto,Shin-ichi Tsukamoto

Bioorganic & Medicinal Chemistry（2012）

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摘要

A series of 4H-1,2,4-triazole derivatives with heteroaromatic rings at the 4-position were synthesized as selective GlyT1 inhibitors. The modification of 5 led to identification of 15 with improved selectivity, solubility, and in vivo activity.

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关键词

GlyT1,GlyT2,The NMDA receptors,Schizophrenia,Triazole

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