Synthesis and biological evaluation of novel 1-deoxy-1-[6-[((hetero)arylcarbonyl)hydrazino]-9H-purin-9-yl]-N-ethyl-β-D-ribofuranuronamide derivatives as useful templates for the development of A2B adenosine receptor agonists

被引：21

作者：

Baraldi, Pier Giovanni ^{[1
]}

Preti, Delia

Tabrizi, Mojgan Aghazadeh

Fruttarolo, Francesca

Romagnoli, Romeo

Carrion, Maria Dora

Lopez Cara, Luisa Carlota

Moorman, Allan R.

Varani, Katia

Borea, Pier Andrea

机构：

[1] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy

[2] Univ Ferrara, Dipartimento Med Clin & Sperimentale, Sez Farmacol, I-44100 Ferrara, Italy

[3] King Pharmaceut Res & Dev Inc, Cary, NC 27513 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 50卷 / 02期

关键词：

D O I：

10.1021/jm061170a

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The lack of molecules endowed with selective and potent agonistic activity toward the hA(2B) adenosine receptors has limited the studies on this pharmacological target and consequently the evaluation of its therapeutic potential. We report the design and the synthesis of the first potent (EC50 in the nanomolar range) and selective hA(2B) adenosine receptor agonists consisting of 1-deoxy-1-[6-[((hetero)arylcarbonyl)hydrazino]-9H-purin-9-yl]-N-ethyl-beta-D-ribofuranuronamide derivatives. The concurrent effect of 6-substitution of the purine nucleus with a ((hetero)arylcarbonyl)hydrazino function and a 2-chloro substitution has been investigated in such NECA derivatives.

引用

页码：374 / 380

页数：7

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