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The rational development of small molecule tachykinin NK3 receptor selective antagonists - the utilisation of a dipeptide chemical library in drug design

1994; Elsevier BV; Volume: 4; Issue: 14 Linguagem: Inglês

10.1016/s0960-894x(00)80360-1

1464-3405

P. Boden, J.M. Eden, Julie Hodgson, David C. Horwell, William Howson, Joel W. Hughes, A.T. McKnight, Ken Meecham, Martyn C. Pritchard, Jennifer Raphy, Giles S. Ratcliffe, Nirmala Suman‐Chauhan, G.N. Woodruff,

Receptor Mechanisms and Signaling

Boc(S)Phe(S)PheNH2 (1c) was identified from the biological screening of an in-house dipeptide chemical library as a micromolar NK3 receptor selective ligand (IC50=1150nM). This lead structure has subsequently been developed into a series of potent and selective NK3 receptor antagonists an example of which is the urea derivative Boc(S)Phe(R)αMePheNH(CH2)7NHCOHNH2 (11d, PD157672) (IC50=16nM).