128950-13-0Relevant academic research and scientific papers
Nitrophenyl derivatives as aldose reductase inhibitors
Costantino, Luca,Ferrari, Anna Maria,Gamberini, Maria Cristina,Rastelli, Giulio
, p. 3923 - 3931 (2007/10/03)
Nitrophenyl derivatives were recently discovered as a new class of ALR2 inhibitors by means of docking and database screening of the National Cancer Institute database of organic molecules. The nitro group was predicted to bind to the Tyr48 and His110 act
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.
