NOVEL ADENOSINE RECEPTOR LIGANDS - 1,3-DISUBSTITUTED[1]BENZOPYRANO[2,3-C]PYRAZOL-4-ONES - SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS

被引：0

作者：

COLOTTA, V ^{[1
]}

CECCHI, L ^{[1
]}

CATARZI, D ^{[1
]}

MELANI, F ^{[1
]}

FILACCHIONI, G ^{[1
]}

MARTINI, C ^{[1
]}

TACCHI, P ^{[1
]}

LUCACCHINI, A ^{[1
]}

机构：

[1] UNIV PISA,IST POLICATTEDRA DISCIPLINE BIOL,I-56100 PISA,ITALY

来源：

RECEPTORS & CHANNELS | 1993年 / 1卷 / 02期

关键词：

ADENOSINE RECEPTOR LIGANDS; BENZOPYRANOPYRAZOLES; STRUCTURE ACTIVITY RELATIONSHIPS; SYNTHESIS;

D O I：

暂无

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of 1,3-disubstituted[1]benzopyrano[2,3-c]pyrazol-4-ones were synthesized and tested in vitro as A1 and A2 adenosine receptor ligands. The binding results and a molecular modelling study indicated that the presence of a proton donor group in the N6-H region of adenosine and the 7-NH region of xanthine, respectively and occupancy of the A2 lipophilic area by a moiety endowed with an electrostatic effect are essential for receptor affinity and A2-selectivity.

引用

页码：111 / 119

页数：9

共 22 条

[1]

Catarzi D., 1992, PHARM PHARM LETT, V2, P74

[2]

CHANTEGREL B, 1983, SYNTHESIS-STUTTGART, P214

[3] 4-OXO-1H-AND-2H-[1]BENZOPYRANO[4,3-C]PYRAZOLES - PREPARATION FROM 4-HYDROXYCOUMARIN OR 3-CHROMONECARBOXYLIC ACID-DERIVATIVES [J].