Synthesis and Biological Characterization of a Series of 2-Sulfonamidebenzamides as Allosteric Modulators of MrgX1.
Synthesis and Biological Characterization of a Series of 2-Sulfonamidebenzamides as Allosteric Modulators of MrgX1.
复制标题
作为 MrgX1 变构调节剂的一系列 2-磺酰胺苯甲酰胺的合成和生物学表征。
DOI：
10.1021/acsmedchemlett.2c00100
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发表时间：
2022
影响因子：
4.2
通讯作者：
Hopkins,CoreyR
中科院分区：
文献类型：
--
作者：
Sharma,Swagat;Peng,Qi;Vadukoot,AnishK;Aretz,ChristopherD;Jensen,AaronA;Wallick,AlexanderI;Dong,Xinzhong;Hopkins,CoreyR
The present study describes our continued efforts in the discovery and characterization of a series of 2-sulfonamidebenzamides as allosteric modulators of MrgX1. MrgX1 has been shown to be an attractive target as a nonopioid receptor for the potential treatment of chronic pain. Working from our original compound, ML382, and utilizing iterative medicinal chemistry, we have identified key halogen substituents that improve MrgX1 potency by ∼8-fold. In addition, we have evaluated the compounds in Tier 1 drug metabolism and pharmacokinetics assays and have identified key compounds that impart improved potency and microsomal stability.
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影响因子：
3.1
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通讯作者：
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影响因子：
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作者：
Melancon, Bruce J.;Hopkins, Corey R.;Wood, Michael R.;Emmitte, Kyle A.;Niswender, Colleen M.;Christopoulos, Arthur;Conn, P. Jeffrey;Lindsley, Craig W.
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影响因子：
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影响因子：
2.6
作者：
Bridges, Thomas M;Morrison, Ryan D;Byers, Frank W;Luo, Shuanghui;Scott Daniels, J
通讯作者：
Scott Daniels, J