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--D-ribofuranuronamide derivs., e.g. I, is reported. The title compds. were prepd. via arom. nucleophilic substitution of 1-deoxy-1-(6-iodo-9H-purin-9-yl)-N-ethyl--D-ribofuranuronamides with arylhydrazides. I was the most potent of the series, and it was confirmed to be a full agonist in a functional assay based on the measurement of its capacity to modulate cAMP levels in CHO cells expressing the hA2B receptor
Synthesis and biological evaluation of novel 1-deoxy-1-[6-[((hetero)arylcarbonyl)hydrazino]-9H-purin-9-yl]-N-ethyl-be ta-D-ribofuranuronamide derivatives as useful templates for the development of A(2B) adenosine receptor agonists
BARALDI, Pier Giovanni;PRETI, Delia;AGHAZADEH TABRIZI, Mojgan;FRUTTAROLO, Francesca;ROMAGNOLI, Romeo;VARANI, Katia;BOREA, Pier Andrea
2007
Abstract
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--D-ribofuranuronamide derivs., e.g. I, is reported. The title compds. were prepd. via arom. nucleophilic substitution of 1-deoxy-1-(6-iodo-9H-purin-9-yl)-N-ethyl--D-ribofuranuronamides with arylhydrazides. I was the most potent of the series, and it was confirmed to be a full agonist in a functional assay based on the measurement of its capacity to modulate cAMP levels in CHO cells expressing the hA2B receptorFile in questo prodotto:
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