Sharma, Swagat; Peng, Qi; Vadukoot, Anish K.; Aretz, Christopher D.; Jensen, Aaron A.; Wallick, Alexander I.; Dong, Xinzhong; Hopkins, Corey R. published the artcile< Synthesis and Biological Characterization of a Series of 2-Sulfonamidebenzamides as Allosteric Modulators of MrgX1>, SDS of cas: 10541-78-3, the main research area is sulfonamidebenzamide preparation allosteric modulator protein coupled receptor.
The present study describes the continued efforts in the discovery and characterization of a series of 2-sulfonamidebenzamides e.g., 3-(Cyclopropanesulfonamido)-N-(2-ethoxyphenyl)-2-naphthamide 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 the original compound, ML382, and utilizing iterative medicinal chem., key halogen substituents that improve MrgX1 potency by ~8-fold were identified. In addition, the compounds in Tier 1 drug metabolism and pharmacokinetics assays were evaluated and the key compounds that impart improved potency and microsomal stability were identified.
ACS Medicinal Chemistry Letters published new progress about Allosteric modulators. 10541-78-3 belongs to class ethers-buliding-blocks, and the molecular formula is C8H11NO, SDS of cas: 10541-78-3.
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem