| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371974 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
We describe here the discovery and biological profile of a series of isoindolinone derivatives as developed mGluR1 antagonists. Our combined strategy of rapid parallel synthesis and conventional medicinal optimization successfully led to N-cyclopropyl 22 and N-isopropyl isoindolinone analogs 21 and 23 with improved in vivo DMPK profiles. Moreover the most advanced analog 23 showed an oral antipsychotic-like effect at a dose of 1 mg/kg in an animal model.
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Related Topics
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Chemistry
Organic Chemistry
Authors
Satoru Ito, Yukari Hirata, Yasushi Nagatomi, Atsushi Satoh, Gentaroh Suzuki, Toshifumi Kimura, Akio Satow, Shunsuke Maehara, Hirohiko Hikichi, Mikiko Hata, Hisashi Ohta, Hiroshi Kawamoto,