Development of highly potent phosphodiesterase 10A (PDE10A) inhibitors: Synthesis and in vitro evaluation of 1,8-dipyridinyl- and 1-pyridinyl-substituted imidazo[1,5-a]quinoxalines
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- 作者：Sally Wagnera ; s.wagner@hzdr.de" class="auth_mail" title="E-mail the corresponding author ; Matthias Scheunemanna ; Karolin Dippera ; Ute Egerlandb ; Norbert Hoefgenb ; Jö ; rg Steinbacha ; Peter Brusta
- 关键词：PDE10A inhibitor ; Imidazo[1 ; 5-a]quinoxalines ; PDE10A imaging agent
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：1 January 2016
- 年：2016
- 卷：107
- 期：Complete
- 页码：97-108
- 全文大小：1053 K
文摘
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Novel fluorinated imidazo[1,5-a]quinoxaline derivatives were synthesized.
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The strategy allows a diversity oriented synthesis (DOS).
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Compounds were evaluated as potent inhibitors of PDE10A.
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2-F-pyridin-3-yl as substituent lead to highly potent (picomolar IC50) inhibitors.
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A high selectivity for PDE10A was found for bromine-containing analogs.