Synthesis of 1-arylpiperazyl-2-phenylcyclopropanes designed as antidopaminergic agents: cyclopropane-based conformationally restricted analogs of haloperidol.
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Yamaguchi K, Kazuta Y, Hirano K, Yamada S, Matsuda A, Shuto S
Synthesis of 1-arylpiperazyl-2-phenylcyclopropanes designed as antidopaminergic agents: cyclopropane-based conformationally restricted analogs of haloperidol.
Bioorg Med Chem. 2008 Oct 1;16(19):8875-81. doi: 10.1016/j.bmc.2008.08.061. Epub 2008 Aug 29.
- PubMed ID
- 18793859 [ View in PubMed]
- Abstract
A series of the cyclopropane-based conformationally restricted analogs of haloperidol were designed as potential antidopaminergic agents and were effectively synthesized using highly stereoselective Grignard reaction with tert-butanesulfinyl imines as the key step. Pharmacological evaluation of the compounds showed that the conformational restriction method can effectively work for improving the pharmacological selectivity of a parent compound and also for investigating the bioactive conformation.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Haloperidol Dopamine D2 receptor Ki (nM) 5.09 N/A N/A Details