ALIPHATIC REPLACEMENTS OF THE BIPHENYL MOIETY OF THE NONPEPTIDYL GROWTH-HORMONE SECRETAGOGUES L-692,429 AND L-692,585

被引：7

作者：

CHU, L ^{[1
]}

MROZIK, H ^{[1
]}

FISHER, MH ^{[1
]}

BROWN, JE ^{[1
]}

CHENG, K ^{[1
]}

CHAN, WWS ^{[1
]}

SCHOEN, WR ^{[1
]}

WYVRATT, MJ ^{[1
]}

BUTLER, BS ^{[1
]}

SMITH, RG ^{[1
]}

机构：

[1] MERCK & CO INC,MERCK SHARP & DOHME RES LABS,DEPT BIOCHEM & PHYSIOL,RAHWAY,NJ 07065

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 19期

关键词：

D O I：

10.1016/0960-894X(95)00389-B

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Replacement of the central phenyl ring of the biphenyl moiety in the novel growth hormone (GH) secretagogues L-692,429 and L-692,585 with partially or completely saturated surrogates has been investigated. The cyclohexenyl analogue 37 displayed GH releasing activity comparable to L-692,585, indicating that the aromaticity of this central ring is not critical for bioactivity and that this ring may serve primarily to orient the benzolactam and phenyltetrazole pharmacophores.

引用

页码：2245 / 2250

页数：6

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