Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species

M Lyles-Eggleston, R Altundas, J Xia…

Index: Lyles-Eggleston; Altundas; Xia; Sikazwe; Fan; Yang; Li; Zhang; Zhu; Schmidt; Vanase-Frawley; Shrihkande; Villalobos; Borne; Ablordeppey Journal of Medicinal Chemistry, 2004 , vol. 47, # 3 p. 497 - 508

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Citation Number: 38

Abstract

The long-term, irreversible, Parkinsonism-like side effects of haloperidol have been speculated to involve several mechanisms. More recently, it has been speculated that the metabolic transformation to MPP+-like species may contribute to the Parkinsonism-like side effects. Because BCPP+ and its reduced analogue have been shown to possess the potential to destroy dopamine receptors in the nigrostriatum, we have designed new ...

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Synthesis and structure-activity relationships for a series ...

[Burkholder, Timothy P.; Kudlacz, Elizabeth M.; Maynard, George D.; Liu, Xiao-Gao; Le, Tieu-Binh; Webster, Mark E.; Horgan, Stephen W.; Wenstrup, David L.; Freund, David W.; Boyer, Fred; Bratton, Larry; Gross, Raymond S.; Knippenberg, Robert W.; Logan, Deborah E.; Jones, Bryan K.; Chen, Teng-Man; Geary, Julie L.; Correll, Melinda A.; Poole, J. Chuck; Mandagere, Arun K.; Thompson, Thomas N.; Hwang, Kin-Kai Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 19 p. 2531 - 2536]