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

RR Goehring, JFW Whitehead, K Brown, K Islam…

文献索引：Goehring, R. Richard; Whitehead, John F.W.; Brown; Islam, Khondaker; Wen, Xin; Zhou, Xiaoming; Chen, Zhengming; Valenzano, Kenneth J.; Miller, Wendy S.; Shan, Shen; Kyle, Donald J. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 20 p. 5045 - 5050

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被引用次数: 16

摘要

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 GTPγ [35S] binding.