Document Report Card

ID: ALA1649068

Journal: J Med Chem

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

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.

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.

CiteXplore: 21141920

DOI: 10.1021/jm101031u