Author/Authors :
Gregory A. Reichard، نويسنده , , James Spitler، نويسنده , , Robert Aslanian، نويسنده , , Mwangi wa Mutahi، نويسنده , , Neng-Yang Shih، نويسنده , , Ling Lin، نويسنده , , Pauline C. Ting، نويسنده , , John C. Anthes، نويسنده , , John J. Piwinski، نويسنده ,
Abstract :
A thorough SAR study of the oxime region of the dual NK1/NK2 antagonist 1 revealed several modifications that result in potent dual antagonists. Follow up SAR studies on a second-generation scaffold demonstrate that certain polar groups on the oxime can improve the dual binding affinity to the subnanomolar range.