Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 17, Pages 5011-5013Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.06.032
Keywords
Sigma receptors; Benzothiazolone; 96 Well
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Funding
- National Institute of Drug Abuse [DA023205, DA013978]
- National Institute of General Medicine [GM014932]
- National Center for Research Resources, National Institutes of Health [C06 RR-13503-01]
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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 (sigma) ligands. Many compounds in this series displayed low nanomolar affinity for the sigma receptor subtypes. In particular, 8a showed high affinity (sigma-1 K-i = 4.5 nM) for sigma-1 receptors and moderately high selectivity (483-fold) over sigma-2 receptors. (C) 2013 Elsevier Ltd. All rights reserved.
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