Structure-activity relationship study of novel NR2B-selective antagonists with arylamides to avoid reactive metabolites

被引：11
|
作者：
Kawai, Makoto
Sakurada, Isao
Morita, Asato
Iwamuro, Yuko
Ando, Kazuo
Omura, Hirofumi
Sakakibara, Sachiko
Masuda, Tsutomu
Koike, Hiroki
Honma, Teruki
Hattori, Kazunari
Takashima, Tadayuki
Mizuno, Kunihiko
Mizutani, Mayumi
Kawamura, Mitsuhiro
机构：
[1] Pfizer Global Res & Dev, Nagoya Labs, Discovery Chem, Aichi 4702393, Japan
[2] Pfizer Global Res & Dev, Nagoya Labs, Pharmacokinet Dynam & Metab, Aichi 4702393, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 20期
关键词：
reactive metabolite; bioactivation; NR2B; NMDA; metabolic stability;
D O I：
10.1016/j.bmcl.2007.08.033
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A novel potent NMDA-NR2B selective antagonist (5b) without the reactive metabolites formation issue was identified. Through this study, a close correlation between reactive metabolites formation and calculated HOMO energies of parent compounds was found. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5537 / 5542
页数：6
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