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

Abstract：

:The lack of molecules endowed with selective and potent agonistic activity toward the hA2B 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 hA2B 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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Baraldi PG,Preti D,Tabrizi MA,Fruttarolo F,Romagnoli R,Carrion MD,Cara LC,Moorman AR,Varani K,Borea PA

doi

10.1021/jm061170a

subject

Has Abstract

pub_date

2007-01-25 00:00:00

pages

374-80

issue

2

eissn

0022-2623

issn

1520-4804

journal_volume

50

pub_type

杂志文章

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