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- W2072387777 abstract "New A3 adenosine receptor antagonists were synthesized and tested at human adenosine receptor subtypes. An advanced synthetic strategy permitted us to obtain a large amount of the key intermediate 5 that was then submitted to alkylation procedures in order to obtain the derivatives 6–8. These compounds were then functionalised into ureas at the 5-position (compounds 9–11, 18 and 19) to evaluate their affinity and selectivity versus hA3 adenosine receptor subtype; in particular, compounds 18 and 19 displayed a value of affinity of 4.9 and 1.3 nM, respectively. Starting from 5, the synthetic methodologies employed permitted us to perform a rapid and a convenient divergent synthesis. A further improvement allowed the regioselective preparation of the N8-substituted compound 7. This method could be used as an helpful general procedure for the design of novel A3 adenosine receptor antagonists without the difficulty of separating the N8-substituted pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidines from the corresponding N7-isomers." @default.
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- W2072387777 date "2003-09-15" @default.
- W2072387777 modified "2023-10-02" @default.
- W2072387777 title "New strategies for the synthesis of A3 adenosine receptor antagonists" @default.
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- W2072387777 doi "https://doi.org/10.1016/s0968-0896(03)00484-x" @default.
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