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ChemInform Abstract: Spiro-Substituted Piperidines as Neurokinin Receptor Antagonists. Part 3. Synthesis of (.+-.)-N-[2-(3,4-Dichlorophenyl)-4-(spiro-substituted piperidin-1′-yl)butyl]-N-methylbenzamides and Evaluation of NK1—NK2 Dual Antagonistic Activities.

✍ Scribed by Hirokazu Kubota; ET AL. ET AL.

Publisher
John Wiley and Sons
Year
2010
Weight
36 KB
Volume
30
Category
Article
ISSN
0931-7597

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✦ Synopsis

Spiro-Substituted Piperidines as Neurokinin Receptor Antagonists. Part 3. Synthesis of (±)-N-[2-(3,4-Dichlorophenyl)-4-(spiro-substituted piperidin-1'-yl)butyl]-N-methylbenzamides and Evaluation of NK 1 -NK 2 Dual Antagonistic Activities. -In order to obtain more potent NK 1 -NK 2 dual antagonists a novel series of the title spiro compounds such as (III) and (VII) are prepared. Among them the derivative (VIIb) (YM-44778) is the most potent and balanced compound concerning both receptor types. The structure-activity relationships are discussed. -(KUB-

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✍ Richard M. Woodward; et al. et al. 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 38 KB

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