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嘌呤并[7,8-c]喹唑啉-8,10(9H,11H)-二酮作为8-芳基黄嘌呤的刚性类似物的合成及其对A1-腺苷受体的亲和力

Synthesis and A1-adenosine receptors affinities of purino[7,8-c]quinazoline-8,10(9H,11H)-diones as rigid analogues of 8-arylxanthines.

作者信息

Ceccarelli S, D'Alessandro A, Magnante F, Scuri R, Zanarella S

机构信息

Centro Ricerche del Consorzio Biomedica Foscama-Irfi, Ferentino, Italia.

出版信息

Farmaco. 1993 Sep;48(9):1301-12.

PMID:8259987
Abstract

Title compounds were prepared by a cyclocondensation reaction between 8-(2-aminophenyl)xanthines and trialkyl orthoesters. Some of them showed activities as A1-adenosine receptor antagonists with binding values in the micromolar range. Results are discussed with reference to 1,3-dialkyl-8-arylxanthines. Considerations on the role played by both electronic and conformational factors are also reported.

摘要

通过8-(2-氨基苯基)黄嘌呤与原酸三烷基酯之间的环缩合反应制备了标题化合物。其中一些化合物表现出作为A1-腺苷受体拮抗剂的活性，其结合值在微摩尔范围内。参考1,3-二烷基-8-芳基黄嘌呤对结果进行了讨论。还报道了关于电子和构象因素所起作用的考量。

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