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Carbamate ester derivatives as potential prodrugs of the presynaptic dopamine autoreceptor agonist (-)-3-(3-hydroxyphenyl)-N-propylpiperidine

…, D Sanchez, P Lindberg, JLG Nilsson

文献索引:Thorberg; Berg; Lundstrom; Pettersson; Wijkstrom; Sanchez; Lindberg; Nilsson Journal of Medicinal Chemistry, 1987 , vol. 30, # 11 p. 2008 - 2012

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被引用次数: 31

摘要

Twenty derivatives bearing substituents on the phenolic function of (-)-3-(3-hydroxyphenyl)- N-propylpiperidine [(-)-3-PPP] were synthesized and tested as prodrugs. The carbamate ester derivatives were found to be the most suitable prodrugs, and especially the 4- isopropylphenylcarbamate 20 was capable of escaping the first-pass metabolism and still generating high plasma levels of the parent compound. Four hours after an oral dose of ...