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

Bhat, Rohit;Fishback, James A;Matsumoto, Rae R;Poupaert, Jacques H.;McCurdy, Christopher R
(2013) Bioorganic & Medicinal Chemistry Letters : the tetrahedron journal for research at the interface of chemistry and biology — Vol. 23, n° 17, p. 5011-5013 (2013)

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Authors
  • Bhat, Rohit
    Author
  • Fishback, James A
    Author
  • Matsumoto, Rae R
    Author
  • Poupaert, Jacques H.UCLouvain
    Author
  • McCurdy, Christopher R
    Author
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.
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Bhat, R., Fishback, J. A., Matsumoto, R. R., Poupaert, J. H., & McCurdy, C. R. (2013). Structure activity relationship study of benzo[d]thiazol-2(3H)one based σ receptor ligands. Bioorganic & Medicinal Chemistry Letters : the tetrahedron journal for research at the interface of chemistry and biology, 23(17), 5011-5013. https://doi.org/10.1016/j.bmcl.2013.06.032 (Original work published 2013)