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Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.

Abstract：

: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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Peprah K,Zhu XY,Eyunni SV,Setola V,Roth BL,Ablordeppey SY

doi

10.1016/j.bmc.2011.12.019

subject

Has Abstract

pub_date

2012-02-01 00:00:00

pages

1291-7

issue

3

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(11)01025-X

journal_volume

20

pub_type

杂志文章

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