Discovery of novel chiral diazepines as bombesin receptor subtype-3 (BRS-3) agonists with low brain penetration
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- 作者：Tetsuyoshi Matsufuji ; Kousei Shimada ; Shozo Kobayashi ; Asuka Kawamura ; Teppei Fujimoto ; Tsuyoshi Arita ; Takashi Hara ; Masahiro Konishi ; Rie Abe-Ohya ; Masanori Izumi ; Yoshitaka Sogawa ; Youko Nagai ; Kazuhiro Yoshida ; Hisashi Takahashi
- 关键词：Bombesin receptor subtype-3 (BRS-3) agonists ; Diazepine ; Brain penetration
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：1 February, 2014
- 年：2014
- 卷：24
- 期：3
- 页码：750-755
- 全文大小：1440 K
文摘
The discovery and optimization of a novel series of BRS-3 agonists are described. We explored a potent BRS-3 agonist with low brain penetration to avoid an adverse effect derived from central nervous system exposure. Through the derivatization process, chiral diazepines 9f and 9g were identified as possessing low brain penetration as well as potent in vitro activity against human and mouse BRS-3s.