Thiazoles and thiopyridines: novel series of high affinity h5HT(7) ligands.
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.
Thomson
Christopher G
CG
Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Harlow, Essex CM20 2QR, UK. christopher_thomson@merck.com
Beer
Margaret S
MS
Curtis
Neil R
NR
Diggle
Helen J
HJ
Handford
Emma
E
Kulagowski
Janusz J
JJ
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
D008024:Ligands; D011725:Pyridines; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists; D013844:Thiazoles; C078730:serotonin 5 receptor; D012701:Serotonin; D001618:beta-Lactamases