Compounds > 3-((2-methyl-1-3-thiazol-4-yl)ethynyl)piperidine

3-((2-methyl-1-3-thiazol-4-yl)ethynyl)piperidine and Central-Nervous-System-Diseases

3-((2-methyl-1-3-thiazol-4-yl)ethynyl)piperidine has been researched along with Central-Nervous-System-Diseases* in 1 studies

Other Studies

1 other study(ies) available for 3-((2-methyl-1-3-thiazol-4-yl)ethynyl)piperidine and Central-Nervous-System-Diseases

Article	Year
4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate. Bioorganic & medicinal chemistry letters, 2016, Feb-15, Volume: 26, Issue:4 High throughput screening of our corporate compound library followed by hit-to-lead development resulted in a 4-aryl-3-arylsulfonyl-quinoline derivative lead (2) with mGluR5 negative allosteric modulator activity. During the lead optimization process, our objective was to improve affinity and metabolic stability. Modifications at the three targeted regions of the lead structure resulted in compounds with nanomolar affinity and acceptable metabolic stability. One of the most promising compounds (3), showing excellent in vivo efficacy, was selected for preclinical development and subsequent phase I clinical studies. Topics: Allosteric Regulation; Animals; Central Nervous System Diseases; High-Throughput Screening Assays; Humans; Protein Binding; Quinolines; Rats; Receptor, Metabotropic Glutamate 5; Structure-Activity Relationship	2016

Article

Year

4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate.

Bioorganic & medicinal chemistry letters, 2016, Feb-15, Volume: 26, Issue:4

High throughput screening of our corporate compound library followed by hit-to-lead development resulted in a 4-aryl-3-arylsulfonyl-quinoline derivative lead (2) with mGluR5 negative allosteric modulator activity. During the lead optimization process, our objective was to improve affinity and metabolic stability. Modifications at the three targeted regions of the lead structure resulted in compounds with nanomolar affinity and acceptable metabolic stability. One of the most promising compounds (3), showing excellent in vivo efficacy, was selected for preclinical development and subsequent phase I clinical studies.

Topics: Allosteric Regulation; Animals; Central Nervous System Diseases; High-Throughput Screening Assays; Humans; Protein Binding; Quinolines; Rats; Receptor, Metabotropic Glutamate 5; Structure-Activity Relationship

2016