Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl)ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7.2) opener for the treatment of neuropathic pain

被引：12

作者：

Wu, Yong-Jin ^{[1
]}

Conway, Charles M. ^{[1
]}

Sun, Li-Qiang ^{[1
]}

Machet, Frederic ^{[1
]}

Chen, Jie ^{[1
]}

Chen, Ping ^{[1
]}

He, Huan ^{[1
]}

Bourin, Clotilde ^{[1
]}

Calandra, Vincenzo ^{[1
]}

Polino, Joseph L. ^{[1
]}

Davis, Carl D. ^{[1
]}

Heman, Karen ^{[1
]}

Gribkoff, Valentin K. ^{[1
]}

Boissard, Christopher G. ^{[1
]}

Knox, Ronald J. ^{[1
]}

Thompson, Mark W. ^{[1
]}

Fitzpatrick, William ^{[1
]}

Weaver, David ^{[1
]}

Harden, David G. ^{[1
]}

Natale, Joanne ^{[1
]}

Dworetzky, Steven I. ^{[1
]}

Starrett, John E., Jr. ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Res & Dev, Wallingford, CT 06492 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 22期

关键词：

KCNQ2; Kv7.2; Neuropathic pain; Diabetic neuropathy; Acrylamide; CHANNEL MODULATORS; ACRYLAMIDES; RAT; EPILEPSY; MODEL;

D O I：

10.1016/j.bmcl.2013.08.092

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Acrylamide (S)-6, a potent and efficacious KCNQ2 (Kv7.2) opener, demonstrated significant activity in two models of neuropathic pain and in the formalin test, suggesting that KCNQ2 openers may be useful in the treatment of neuropathic pain including diabetic neuropathy. (c) 2013 Elsevier Ltd. All rights reserved.

引用

页码：6188 / 6191

页数：4

共 4 条

[1] (S,E)-N-[1-(3-Heteroarylphenyl)ethyl]-3-(2-fluorophenyl)- acrylamides:: synthesis and KCNQ2 potassium channel opener activity
L'Heureux, A
Martel, A
He, H
Chen, J
Sun, LQ
Starrett, JE
Natale, J
Dworetzky, SI
Knox, RJ
Harden, DG
Weaver, D
Thompson, MW
Wu, YJ
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (02) : 363 - 366
[2] Synthesis and KCNQ2 opener activity of N-(1-benzo[1,3]dioxol-5-yl-ethyl, N-[1-(2,3-dihydro-benzofuran-5-yl)-ethyl, and N-[1-(2,3-dihydro-1H-indol-5-yl)-ethyl acrylamides
Wu, YJ
Sun, LQ
He, H
Chen, J
Starrett, JE
Dextraze, P
Daris, JP
Boissard, CG
Pieschl, RL
Gribkoff, VK
Natale, J
Knox, RJ
Harden, DG
Thompson, MW
Fitzpatrick, W
Weaver, D
Wu, DD
Gao, Q
Dworetzky, SI
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2004, 14 (17) : 4533 - 4537
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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021, 223

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