Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents
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DOI：
10.1016/j.bmc.2011.12.019
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发表时间：
2012-02-01
影响因子：
3.5
通讯作者：
Ablordeppey, Seth Y.
中科院分区：
文献类型：
--
作者：
Peprah, Kwakye;Zhu, Xue Y.;Ablordeppey, Seth Y.
使用氟哌啶醇作为支架，新的代理商被设计成调查的结构贡献的不同群体结合在中枢神经系统受体与非典型抗精神病药物药理学。很明显，每个药效基团，丁酰苯，哌啶和4-氯苯基部分有助于改变与感兴趣的受体的结合。该策略导致鉴定出几种新的药剂，化合物16、18、19、23、24和25，其结合特征满足我们所述的用作潜在的非典型抗精神病药的药剂的标准。这项研究表明，氟哌啶醇可以作为一个有用的领导，在识别和设计新的代理人，目标与抗精神病药物相关的多种受体。爱思唯尔有限公司出版
Using haloperidol as a scaffold, new agents were designed to investigate the structural contributions of various groups to binding at CNS receptors associated with atypical antipsychotic pharmacology. It is clear that each pharmacophoric group, the butyrophenone, the piperidine and the 4-chlorophenyl moieties contributes to changes in binding to the receptors of interest. This strategy has resulted in the identification of several new agents, compounds 16, 18, 19, 23, 24 and 25, with binding profiles which satisfy our stated criteria for agents to act as potential atypical antipsychotics. This research demonstrates that haloperidol can serve as a useful lead in the identification and design of new agents that target multiple receptors associated with antipsychotic pharmacology. Published by Elsevier Ltd.