Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists

…, N Suman-Chauhan, GN Woodruff

Index: Boden, Phil; Eden, Jon M.; Hodgson, Julie; Horwell, David C.; Hughes, John; McKnight, Alexander T.; Lewthwaite, Russell A.; Pritchard, Martyn C.; Raphy, Jenny; Meecham, Ken; Ratcliffe, Giles S.; Suman-Chauhan, Nirmala; Woodruff, Geoffrey N. Journal of Medicinal Chemistry, 1996 , vol. 39, # 8 p. 1664 - 1675

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Citation Number: 47

Abstract

The use of a dipeptide library as the source of a micromolar chemical lead compound for the human tachykinin NK3 receptor is described. The screening of a dipeptide library through a cloned human NK3 receptor binding assay resulted in the identification of Boc (S) Phe (S) PheNH2 (1), which has subsequently been developed, following a'peptoid'design strategy, into a series of high-affinity NK3 receptor selective antagonists. The structure-activity ...