td-5108 and benzimidazole

td-5108 has been researched along with benzimidazole* in 1 studies

Other Studies

1 other study(ies) available for td-5108 and benzimidazole

Article	Year
Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties. Bioorganic & medicinal chemistry letters, 2013, Jul-15, Volume: 23, Issue:14 The discovery of a series of 5-HT4 receptor agonists based on a novel 2-alkylbenzimidazole aromatic core is described. Optimization of the 2-substituent of the benzimidazole ring led to a series of agonists with subnanomolar binding affinity and moderate-to-high intrinsic activity relative to that of 5-HT. Consistent with our previously described multivalent design approach to this target, subsequent optimization of the linker and secondary binding group regions of the series afforded compound 18 (TD-8954), a potent and selective 5-HT4 receptor agonist in vitro with demonstrated prokinetic activity in multiple species. Topics: Animals; Benzimidazoles; Crystallography, X-Ray; Dogs; Drug Evaluation, Preclinical; Guinea Pigs; Half-Life; Intestinal Mucosa; Male; Molecular Conformation; Piperidines; Protein Isoforms; Rats; Rats, Sprague-Dawley; Receptors, Serotonin, 5-HT4; Serotonin 5-HT4 Receptor Agonists	2013

Article

Year

Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties.

Bioorganic & medicinal chemistry letters, 2013, Jul-15, Volume: 23, Issue:14

The discovery of a series of 5-HT4 receptor agonists based on a novel 2-alkylbenzimidazole aromatic core is described. Optimization of the 2-substituent of the benzimidazole ring led to a series of agonists with subnanomolar binding affinity and moderate-to-high intrinsic activity relative to that of 5-HT. Consistent with our previously described multivalent design approach to this target, subsequent optimization of the linker and secondary binding group regions of the series afforded compound 18 (TD-8954), a potent and selective 5-HT4 receptor agonist in vitro with demonstrated prokinetic activity in multiple species.

Topics: Animals; Benzimidazoles; Crystallography, X-Ray; Dogs; Drug Evaluation, Preclinical; Guinea Pigs; Half-Life; Intestinal Mucosa; Male; Molecular Conformation; Piperidines; Protein Isoforms; Rats; Rats, Sprague-Dawley; Receptors, Serotonin, 5-HT4; Serotonin 5-HT4 Receptor Agonists

2013