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Structure activity relationship study of benzo[d]thiazol-2(3H)one based ? 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 (?) ligands. Many compounds in this series displayed low nanomolar affinity for the ? receptor subtypes. In particular, 8a showed high affinity (?-1 Ki = 4.5 nM) for ?-1 receptors and moderately high selectivity (483-fold) over ?-2 receptors.

SUBMITTER: Bhat R

PROVIDER: S-EPMC3762478 | biostudies-literature | 2013 Sep

REPOSITORIES: biostudies-literature

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Structure activity relationship study of benzo[d]thiazol-2(3H)one based σ receptor ligands.

Bhat Rohit R Fishback James A JA Matsumoto Rae R RR Poupaert Jacques H JH McCurdy Christopher R CR

Bioorganic & medicinal chemistry letters 20130629 17

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. ...[more]

PMID: 23867168

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