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

Citation
Ljs. Knutsen et al., THE SYNTHESIS AND BIOCHEMICAL EVALUATION OF NEW A(1) SELECTIVE ADENOSINE RECEPTOR AGONISTS CONTAINING 6-HYDRAZINOPURINE MOIETIES, Bioorganic & medicinal chemistry letters, 3(12), 1993, pp. 2661-2666
Citations number
29
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
ISSN journal
0960894X
Volume
3
Issue
12
Year of publication
1993
Pages
2661 - 2666
Database
ISI
SICI code
0960-894X(1993)3:12<2661:TSABEO>2.0.ZU;2-J
Abstract
The synthesis and SAR of a series of novel derivatives of N-aminoadeno sine is described, along with their in vitro effects in biochemical as says. The rat brain A1 adenosine receptor binding of these compounds i s very dependent upon the purine 2-substituent. The novel agonist, -ch loro-N-[4-(phenylthio)-1-piperidinyl]adenosine, exhibits a K(i) value for A1 receptor binding of <1 nM.