Journal article
Biphenyl derivatives as novel dual NK 1/NK 2-receptor antagonists
R Mah, M Gerspacher, A Von Sprecher, S Stutz, V Tschinke, GP Anderson, C Bertrand, N Subramanian, HA Ball
Bioorganic and Medicinal Chemistry Letters | PERGAMON-ELSEVIER SCIENCE LTD | Published : 2002
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 NK 1 receptor (<10 nM) and for the NK 2 receptor (<50 nM). Details on the design, synthesis, biological activities, SAR and conformational analysis of this new class of dual NK 1/NK 2 receptor antagonists are presented. © 2002 Elsevier Science Ltd. All rights reserved.