Synthesis and evaluation of amides surrogates of dopamine D3 receptor ligands
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- 作者：Mickaë ; l Jean ; Jacques Renault ; Nicolas Levoin ; Denis Danvy ; Thierry Calmels ; Isabelle Berrebi-Bertr ; Philippe Robert ; J.C. Schwartz ; J.M. Lecomte ; Philippe Uriac ; Marc Capet
- 关键词：Dopamine D3 receptor ligand ; Amide isoster ; Selectivity
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：15 September 2010
- 年：2010
- 卷：20
- 期：18
- 页码：5376-5379
- 全文大小：413 K
文摘
Isosteric replacement of the amide function and modulation of the arylpiperazine moiety of known dopamine D3 receptor ligands led to potent and selective compounds. Enhanced bioavailability and preferential brain distribution make compound 6c a good candidate for pharmacological and clinical evaluation.