THE RATIONAL DEVELOPMENT OF SMALL-MOLECULE TACHYKININ NK(3) RECEPTOR-SELECTIVE ANTAGONISTS - THE UTILIZATION OF A DIPEPTIDE CHEMICAL LIBRARY IN DRUG DESIGN

被引：30

作者：

BODEN, P ^{[1
]}

EDEN, JM ^{[1
]}

HODGSON, J ^{[1
]}

HORWELL, DC ^{[1
]}

HOWSON, W ^{[1
]}

HUGHES, J ^{[1
]}

MCKNIGHT, AT ^{[1
]}

MEECHAM, K ^{[1
]}

PRITCHARD, MC ^{[1
]}

RAPHY, J ^{[1
]}

RATCLIFFE, GS ^{[1
]}

SUMANCHAUHAN, N ^{[1
]}

WOODRUFF, GN ^{[1
]}

机构：

[1] PARKE DAVIS NEUROSCI RES CTR,ADDENBROOKES HOSP SITE,HILLS RD,CAMBRIDGE CB2 2QB,ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(00)80360-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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=1550nM). 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)alphaMePheNH(CH2)7NHCONH2 (11d, PD157672) (IC50=16nM).

引用

页码：1679 / 1684

页数：6

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