Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological …

…, AJ Robichaud, T Lee, J Tomesch, W Yao…

Index: Li, Peng; Zhang, Qiang; Robichaud, Albert J.; Lee, Taekyu; Tomesch, John; Yao, Wei; Beard, J. David; Snyder, Gretchen L.; Zhu, Hongwen; Peng, Youyi; Hendrick, Joseph P.; Vanover, Kimberly E.; Davis, Robert E.; Mates, Sharon; Wennogle, Lawrence P. Journal of Medicinal Chemistry, 2014 , vol. 57, # 6 p. 2670 - 2682

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Citation Number: 14

Abstract

We report the synthesis and structure–activity relationships of a class of tetracyclic butyrophenones that exhibit potent binding affinities to serotonin 5-HT2A and dopamine D2 receptors. This work has led to the discovery of 4-((6b R, 10a S)-3-methyl-2, 3, 6b, 9, 10, 10 a-hexahydro-1 H, 7 H-pyrido [3′, 4′: 4, 5] pyrrolo [1, 2, 3-de] quinoxalin-8-yl)-1-(4- fluorophenyl)-butan-1-one 4-methylbenzenesulfonate (ITI-007), which is a potent 5-HT2A ...