Synthesis and Structure-Activity Relationships of Carboxylated Chalcones: A Novel Series of CysLT 1 (LTD4) Receptor Antagonists

ME Zwaagstra, H Timmerman, M Tamura…

Index: Zwaagstra, Mariel E.; Timmerman, Hendrik; Tamura, Masahiro; Tohma, Tsutomu; Wada, Yasushi; Onogi, Kazuhiro; Zhang, Ming-Qiang Journal of Medicinal Chemistry, 1997 , vol. 40, # 7 p. 1075 - 1089

Full Text: HTML

Citation Number: 59

Abstract

The synthesis and CysLT 1 antagonistic activities of a new series of 2-, 3-, and 4-(2- quinolinylmethoxy)-and 3-and 4-[2-(2-quinolinyl) ethenyl]-substituted, 2'-, 3'-, 4'-, or 5'- carboxylated chalcones are described. Structure-activity relationship studies indicate a preference for the presence of a negatively charged (acidic) moiety, although in some cases nitrile or ester analogues also exhibit moderate activity. The quinoline moiety may be ...