Tetracyclic spirooxindole blockers of hNaV1.7: activity in vitro and in CFA-induced inflammatory pain model
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- 作者：Sultan Chowdhury (1)
Shifeng Liu (1)
Jay A. Cadieux (1)
Tom Hsieh (1)
Mikhail Chafeev (1)
Shaoyi Sun (1)
Qi Jia (1)
Jianyu Sun (1)
Mark Wood (1)
Jonathan Langille (1)
Serguei Sviridov (1)
Jianmin Fu (1)
Zaihui Zhang (1)
Ray Chui (2)
Audrey Wang (2)
Xing Cheng (2)
Jing Zhong (2)
Sazzad Hossain (2)
Kuldip Khakh (2)
Ivana Rajlic (2)
Henry Verschoof (2)
Rainbow Kwan (2)
Wendy Young (2) - 关键词：Sodium channel blockers ; NaV1.7 blockers ; Pain ; Tetracyclic spirooxindole ; Methylenedioxy ; Mitsunobu reaction
- 刊名：Medicinal Chemistry Research
- 出版年：2013
- 出版时间：April 2013
- 年：2013
- 卷：22
- 期：4
- 页码：1825-1836
- 全文大小：1209KB
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Shifeng Liu (1)
Jay A. Cadieux (1)
Tom Hsieh (1)
Mikhail Chafeev (1)
Shaoyi Sun (1)
Qi Jia (1)
Jianyu Sun (1)
Mark Wood (1)
Jonathan Langille (1)
Serguei Sviridov (1)
Jianmin Fu (1)
Zaihui Zhang (1)
Ray Chui (2)
Audrey Wang (2)
Xing Cheng (2)
Jing Zhong (2)
Sazzad Hossain (2)
Kuldip Khakh (2)
Ivana Rajlic (2)
Henry Verschoof (2)
Rainbow Kwan (2)
Wendy Young (2)
1. Department of Medicinal Chemistry, Xenon Pharmaceuticals Inc., 3650 Gilmore Way, Burnaby, BC, V5G 4W8, Canada
2. Department of Biological Sciences, Xenon Pharmaceuticals Inc., 3650 Gilmore Way, Burnaby, BC, V5G 4W8, Canada
文摘
The structure–activity relationship of a new series of tetracyclic spirooxindoles led to the discovery of compound 25a, a potent hNaV1.7 blocker with improved ADME properties and in vivo efficacy in the CFA-induced inflammatory pain model.