1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor

Bioorganic & Medicinal Chemistry Letters
R Richard GoehringDonald J Kyle

Abstract

A series of 1,3-dihydro-2,1,3-benzothiadiazol-2,2-diones (I) and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones (II) were prepared. While the five-member ring series (I) did not show good affinity for opioid receptors, the six-member ring series (II) exhibited extremely high affinity and selectivity for the NOP receptor and showed full agonist activity, as determined by stimulation of GTPgamma[35S] binding.

References

Sep 22, 2000·Peptides·C Mollereau, L Mouledous
Apr 10, 2004·Journal of Computer-aided Molecular Design·Britta M BröerHans-Dieter Höltje

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Citations

Nov 9, 2006·Chemistry : a European Journal·Moballigh AhmedMatthias Beller
May 27, 2017·Beilstein Journal of Organic Chemistry·Anna S ZalivatskayaAleksander V Vasilyev
Jan 26, 2010·Medicinal Research Reviews·Carlo Mustazza, Giuditta Bastanzio

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