Synthesis and SAR of aminothiazole fused benzazepines as selective dopamine D 2 partial agonists
…, Y Wu, W Blackwell, G Steelman, J Rosamond…
Index: Urbanek, Rebecca A.; Xiong, Hui; Wu, Ye; Blackwell, William; Steelman, Gary; Rosamond, Jim; Wesolowski, Steven S.; Campbell, James B.; Zhang, Minli; Brockel, Becky; Widzowski, Daniel V. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 2 p. 543 - 547
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Citation Number: 4
Abstract
Dopamine (D2) partial agonists (D2PAs) have been regarded as a potential treatment for schizophrenia patients with expected better side effect profiles than currently marketed antipsychotics. Herein we report the synthesis and SAR of a series of aminothiazole fused benzazepines as selective D2 partial agonists. These compounds have good selectivity, CNS drug-like properties and tunable D2 partial agonism. One of the key compounds, 8h, ...
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