title: Identification of a series of benzoxazoles as potent 5-HT6 ligands.
abstract: As part of our continuing efforts to identify therapeutics for CNS diseases such as schizophrenia and Alzheimer's disease (AD), we have been focused on the 5-HT(6) receptor in order to identify potent and selective ligands as a potential treatment for cognitive dysfunction. Herein we report the identification of a novel series of benzoxazole derivatives as potent 5-HT(6) ligands. The synthesis and detailed SAR of this class of compounds are reported. The compounds have been shown to be full antagonists in a cyclic AMP functional assay.
authors.affiliation: Chemical & Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA. liuk1@wyeth.com
authors.forename: Kevin G
authors.initials: KG
authors.lastname: Liu
authors.forename: Jennifer R
authors.initials: JR
authors.lastname: Lo
authors.forename: Thomas A
authors.initials: TA
authors.lastname: Comery
authors.forename: Guo Ming
authors.initials: GM
authors.lastname: Zhang
authors.forename: Jean Y
authors.initials: JY
authors.lastname: Zhang
authors.forename: Dianne M
authors.initials: DM
authors.lastname: Kowal
authors.forename: Deborah L
authors.initials: DL
authors.lastname: Smith
authors.forename: Li
authors.initials: L
authors.lastname: Di
authors.forename: Edward H
authors.initials: EH
authors.lastname: Kerns
authors.forename: Lee E
authors.initials: LE
authors.lastname: Schechter
authors.forename: Albert J
authors.initials: AJ
authors.lastname: Robichaud
mesh_terms: D001583:Benzoxazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D003072:Cognition Disorders / Q000188:drug therapy*; D020650:Combinatorial Chemistry Techniques; D000242:Cyclic AMP / Q000037:antagonists & inhibitors; D015195:Drug Design; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D011985:Receptors, Serotonin / Q000187:drug effects*; D018490:Serotonin Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D001583:Benzoxazoles; D008024:Ligands; D011985:Receptors, Serotonin; D018490:Serotonin Agents; C097216:serotonin 6 receptor; D000242:Cyclic AMP