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2005
Thiadiazine derivatives
R 0660
1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-Dihydro-1H-2,1,3-benzoas Ligands for the NOP Receptor. — A series of the title thia04- 175 thidiazin-2,2-diones
diazole (VII) and thiadiazine derivatives (XIV)/(XVI) are synthesized and evaluated
for their binding affinity at the human NOP receptor. In vitro screening indicates that
the former five-membered series is not especially active, while the six-membered series
shows excellent affinity and potent agonist activity at the NOP receptor. —
(GOEHRING*, R. R.; et al.; Bioorg. Med. Chem. Lett. 14 (2004) 20, 5045-5050;
Drug Discovery, Purdue Pharma LP, Cranbury, NJ 08512, USA; Eng.) —
M. Schroeter
2005
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