A series of 6-and 7-piperazinyl-and-piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent

…, DJ Wustrow, WA Brink, KT Zoski, YH Shih…

Index: Belliotti, Thomas R.; Wustrow, David J.; Brink, Wouter A.; Zoski, Kim T.; Shih, Yu-Hsin; Whetzel, Steven Z.; Georgic, Lynn M.; Corbin, Ann E.; Akunne, Hyacinth C.; Heffner, Thomas G.; Pugsley, Thomas A.; Wise, Lawrence D. Journal of Medicinal Chemistry, 1999 , vol. 42, # 25 p. 5181 - 5187

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Citation Number: 25

Abstract

As part of a program to develop dopamine D4 antagonists for the treatment of schizophrenia, we discovered a series of 6-and 7-(phenylpiperazinyl)-and-(phenylpiperidinyl) methylbenzoxazinones through mass screening of our compound library. A structure-activity relationship SAR study was carried out involving substituents on the phenyl ring, and several selective D4 antagonists were identified. The 7-substituted benzoxazinones ...