title: Thiazoles and thiopyridines: novel series of high affinity h5HT(7) ligands.
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.
authors.affiliation: Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Harlow, Essex CM20 2QR, UK. christopher_thomson@merck.com
authors.forename: Christopher G
authors.initials: CG
authors.lastname: Thomson
authors.forename: Margaret S
authors.initials: MS
authors.lastname: Beer
authors.forename: Neil R
authors.initials: NR
authors.lastname: Curtis
authors.forename: Helen J
authors.initials: HJ
authors.lastname: Diggle
authors.forename: Emma
authors.initials: E
authors.lastname: Handford
authors.forename: Janusz J
authors.initials: JJ
authors.lastname: Kulagowski
mesh_terms: D002478:Cells, Cultured; D006801:Humans; D008024:Ligands; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011985:Receptors, Serotonin / Q000737:chemistry* / Q000378:metabolism*; D012701:Serotonin / Q000378:metabolism; D017366:Serotonin Receptor Agonists / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D001618:beta-Lactamases / Q000378:metabolism
chemical_list: D008024:Ligands; D011725:Pyridines; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists; D013844:Thiazoles; C078730:serotonin 5 receptor; D012701:Serotonin; D001618:beta-Lactamases