THE SYNTHESIS AND BIOCHEMICAL EVALUATION OF NEW A(1) SELECTIVE ADENOSINE RECEPTOR AGONISTS CONTAINING 6-HYDRAZINOPURINE MOIETIES

被引：16

作者：

KNUTSEN, LJS

LAU, J

SHEARDOWN, MJ

THOMSEN, C

机构：

[1] NOVO NORDISK PHARMACEUT DIV,DEPT NEUROPHARMACOL,DK-2760 MALOV,DENMARK

[2] NOV NORDISK PHARMACEUT DIV,DEPT RECEPTOR NEUROCHEM,DK-2760 MALOV,DENMARK

[3] NOVO NORDISK PHARMACEUT DIV,DEPT DRUG DISCOVERY,DK-2760 MALOV,DENMARK

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(01)80737-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and SAR of a series of novel derivatives of N-aminoadenosine is described, along with their in vitro effects in biochemical assays. The rat brain A1 adenosine receptor binding of these compounds is very dependent upon the purine 2-substituent. The novel agonist, 2-chloro-N-[4-(phenylthio)-1-piperidinyl]adenosine, exhibits a K(i) value for A1 receptor binding of <1 nM.

引用

页码：2661 / 2666

页数：6

共 29 条

[1] PHYSIOLOGICAL AND PHARMACOLOGICAL PROPERTIES OF ADENOSINE - THERAPEUTIC IMPLICATIONS [J].