198271-58-8Relevant articles and documents
Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands
Lee-Dutra, Alice,Arienti, Kristen L.,Buzard, Daniel J.,Hack, Michael D.,Khatuya, Haripada,Desai, Pragnya J.,Nguyen, Steven,Thurmond, Robin L.,Karlsson, Lars,Edwards, James P.,Breitenbucher, J. Guy
, p. 6043 - 6048 (2007/10/03)
A series of 2-arylbenzimidazoles was synthesized and found to bind with high affinity to the human histamine H4 receptor. Structure-activity relationships were investigated through library preparation and evaluation as well as traditional medicinal chemistry approaches, leading to the discovery of compounds with single-digit nanomolar affinity for the H4 receptor.
Butenolide endothelin antagonists with improved aqueous solubility
Patt, William C.,Cheng, Xue-Min,Repine, Joseph T.,Lee, Chet,Reisdorph, Bill R.,Massa, Mark A.,Doherty, Annette M.,Welch, Kathleen M.,Bryant, John W.,Flynn, Michael A.,Walker, Donnelle M.,Schroeder, Richard L.,Haleen, Stephen J.,Keiser, Joan A.
, p. 2162 - 2168 (2007/10/03)
Continued development around our ET(A)-selective endothelin (ET) antagonist 1 (CI-1020) has led to the synthesis of analogues with improved aqueous solubility profiles. Poor solubility characteristics displayed by 1 required a complex buffered formulation