Design and discovery of 1,3-benzodiazepines as novel dopamine antagonists
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- 作者：Zhaoning Zhu ; Zhong-Yue Sun ; Yuanzan Ye ; Brian McKittrick ; William Greenlee ; Michael Czarniecki ; Ahmad Fawzi ; Hongtao Zhang ; Jean E. Lachowicz
- 关键词：Dopamine ; D1 receptor antagonist ; Benzodiazepine
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：1 September 2009
- 年：2009
- 卷：19
- 期：17
- 页码：5218-5221
- 全文大小：1372 K
文摘
A series of novel 1,3-benzodiazapine based D1 antagonists was designed according to the understanding of pharmacophore models derived from SCH 23390 (1b), a potent and selective D1 antagonist. The new design features an achiral cyclic-amidine that maintains desired basicity. Solid phase synthesis was developed for SAR development of the novel dopamine antagonists.