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
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
收藏
页码:2661 / 2666
页数:6
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