Functional probing of the backbone of the Sanofi NK2 antagonist SR 48968 ha
s resulted in the discovery of two new classes of NK1/NK2 dual antagonists:
the diamine class and the oxime class. The addition of the amino or the ox
ime functional group results in the reversal of the stereochemical preferen
ce of the NK2 receptor. (C) 2000 Elsevier Science Ltd. All rights reserved.