Butenolide endothelin antagonists with improved aqueous solubility

…, BR Reisdorph, MA Massa, AM Doherty…

Index: 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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Citation Number: 18

Abstract

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. ...