117424-72-3Relevant academic research and scientific papers
Intermediates for leukotriene antagonists
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, (2008/06/13)
This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, intermediates for preparing the derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
Benzophenone Dicarboxylic Acid Antagonists of Leukotriene B4. 1. Structure-Activity Relationships of the Benzophenone Nucleus
Gapinski, D. Mark,Mallett, Barbara E.,Froelich, Larry L.,Jackson, William T.
, p. 2798 - 2807 (2007/10/02)
A series of lipophilic benzophenone dicarboxylic acid derivatives was prepared which inhibited the binding of the potent chemotaxin leukotriene B4 to its receptor(s) on intact human neutrophils.With a radioligand-binding assay as a measure of receptor affinity, a structure-activity relationship for this series was investigated.Both acidic residues were required for receptor-binding activity.The relative orientation of the two acidic groups was important for optimal binding.Replacement of the carbonyl group of the benzophenone with a variety of polar and nonpolar linking groups lead to only small changes in binding affinity, indicating the linking group may not be involved in receptor recognition.Further structure-activity relationships within this series are reported in an accompanying paper.
