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Discovery of novel chiral diazepines as bombesin receptor subtype-3 (BRS-3) agonists with low brain penetration |
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| Institution: | 1. Crop Protection Division, National Academy of Agricultural Science, RDA, Republic of Korea;2. Greenagrotech, 196-2 Inan-ri, Apryang-meon, Gyungsan, Gyungbuk Province, Republic of Korea;3. Crop Environment Research Division, National Institute of Crop Science, RDA, Republic of Korea;4. Horticultural Environmental Division, National Institute of Horticultural & Herbal Science, RDA, Republic of Korea |
| Abstract: | 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. |
| Keywords: | Bombesin receptor subtype-3 (BRS-3) agonists Diazepine Brain penetration |
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