Author/Authors :
Robert Mah، نويسنده , , Marc Gerspacher، نويسنده , , Andreas von Sprecher، نويسنده , , Stefan Stutz، نويسنده , , Vincenzo Tschinke، نويسنده , , Gary P. Anderson، نويسنده , , Jean Claude Bertrand، نويسنده , , Natarajan Subramanian، نويسنده , , Howard A. Ball، نويسنده ,
Abstract :
In a continuation of our efforts to simplifly the structure of our neurokinin antagonists, a series of substituted biphenyl derivatives has been prepared. Several compounds exhibit potent affinities for both the NK1 receptor (<10 nM) and for the NK2 receptor (<50 nM). Details on the design, synthesis, biological activities, SAR and conformational analysis of this new class of dual NK1/NK2 receptor antagonists are presented.