Butenolide endothelin antagonists with improved aqueous solubility

…, BR Reisdorph, MA Massa, AM Doherty…

文献索引：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. Journal of Medicinal Chemistry, 1999 , vol. 42, # 12 p. 2162 - 2168

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被引用次数: 18

摘要

Continued development around our ETA-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 in order to conduct iv studies. To overcome the use of specific iv formulations for preclinical studies on additional drug candidates, analogues with improved aqueous solubility were desired. ...