Thiazoles and thiopyridines: novel series of high affinity h5HT(7) ligands

Christopher G Thomson; Margaret S Beer; Neil R Curtis; Helen J Diggle; Emma Handford; Janusz J Kulagowski

doi:10.1016/j.bmcl.2003.11.050

Thiazoles and thiopyridines: novel series of high affinity h5HT(7) ligands

Bioorg Med Chem Lett. 2004 Feb 9;14(3):677-80. doi: 10.1016/j.bmcl.2003.11.050.

Authors

Christopher G Thomson¹, Margaret S Beer, Neil R Curtis, Helen J Diggle, Emma Handford, Janusz J Kulagowski

Affiliation

¹ Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Harlow, Essex CM20 2QR, UK. [email protected]

PMID: 14741267
DOI: 10.1016/j.bmcl.2003.11.050

Abstract

A series of thiazole based 5HT(7) ligands has been identified from screening. Optimisation of the pendent aryl group and modification of the core gave a related series of high affinity, selective thiopyridine based 5HT(7) ligands, the most active of which behaves as a partial agonist.

MeSH terms

Cells, Cultured
Humans
Ligands
Pyridines / chemical synthesis*
Pyridines / pharmacology*
Receptors, Serotonin / chemistry*
Receptors, Serotonin / metabolism*
Serotonin / metabolism
Serotonin Receptor Agonists / chemistry
Serotonin Receptor Agonists / pharmacology
Structure-Activity Relationship
Thiazoles / chemical synthesis*
Thiazoles / pharmacology*
beta-Lactamases / metabolism

Substances

Ligands
Pyridines
Receptors, Serotonin
Serotonin Receptor Agonists
Thiazoles
serotonin 5 receptor
Serotonin
beta-Lactamases