Structure activity relationship study of benzo[d]thiazol-2(3H)one based σ receptor ligands
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.
Bhat, Rohit,Fishback, James A.,Matsumoto, Rae R.,Poupaert, Jacques H.,McCurdy, Christopher R.
supporting information
p. 5011 - 5013
(2013/09/02)
Synthesis of 6- and 7-acyl-4H-benzothiazin-3-ones
Synthesis of 6- and 7-substituted benzoxazin-3-ones was already described in the literature by acylation of the corresponding benzoxazin-3-ones or cyclization of the corresponding 4- or 5-acyl-2-aminophenols. This paper describes original synthetic pathwa
AlCl3-DMF Reagent in the Friedel-Crafts Reaction. Application to the Acylation Reaction of 2(3H)-Benzothiazolones
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Yous, Said,Poupaert, Jacques H.,Lesieur, Isabelle,Depreux, Patric,Lesieur, Daniel
p. 1574 - 1576
(2007/10/02)
Benzothiazolinone compounds
Compounds of general formula (I): STR1 in which: R1 represents a hydrogen atom or a lower alkyl group, R2 represents a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstitute
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(2008/06/13)
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