title: Structure activity relationship study of benzo[d]thiazol-2(3H)one based σ receptor ligands.
abstract: Herein we report the SAR study which involved structural modifications to the linker length, aryl substitution and alkylamine ring size of the benzo[d]thiazol-2(3H)one based sigma receptor (σ) ligands. Many compounds in this series displayed low nanomolar affinity for the σ receptor subtypes. In particular, 8a showed high affinity (σ-1 Ki = 4.5 nM) for σ-1 receptors and moderately high selectivity (483-fold) over σ-2 receptors.
authors.affiliation: Department of Medicinal Chemistry, University of Mississippi, University, MS 38677, USA.
authors.forename: Rohit
authors.initials: R
authors.lastname: Bhat
authors.forename: James A
authors.initials: JA
authors.lastname: Fishback
authors.forename: Rae R
authors.initials: RR
authors.lastname: Matsumoto
authors.forename: Jacques H
authors.initials: JH
authors.lastname: Poupaert
authors.forename: Christopher R
authors.initials: CR
authors.lastname: McCurdy
mesh_terms: D000818:Animals; D052160:Benzothiazoles / Q000737:chemistry* / Q000494:pharmacology*; D001665:Binding Sites; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D008024:Ligands; D011485:Protein Binding; D051381:Rats; D017480:Receptors, sigma / Q000378:metabolism*; D013329:Structure-Activity Relationship; D000097605:Sigma-1 Receptor
chemical_list: D052160:Benzothiazoles; D008024:Ligands; D017480:Receptors, sigma; D000097605:Sigma-1 Receptor; C106107:sigma-2 receptor
keywords: 96 Well; Benzothiazolone; Sigma receptors