The aldehyde derivatives of 1,3-dipropyl xanthines as described in this paper, constitutes a new series of selective adenosine ligands displaying bronchospasmolytic activity. The effect of substitution at 3rd - and 4th -position of 8-phenyl xanthine has also been taken into consideration. The synthesized compounds showed varying binding affinities at different adenosine receptor subtypes (A1 , A2A , A2B and A3 ) and also good in vivo bronchospasmolytic activity against histamine aerosol induced asthma in guinea pigs. Most of the compounds showed maximum affinity towards the A2A receptor subtype. The monosubstituted 3-aminoalkoxyl 8-phenyl xanthine with a diethylmoiety (compound 12e) was found to be most potent A2A adenosine receptor ligand (Ki = 0.036 µM) followed by disubstituted 4-aminoalkoxyl-3-methoxy-8-phenyl xanthine (Ki = 0.050µM) (compound 10a).

中文翻译：

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一些较新的 1,3-二丙基-8-苯基取代的黄嘌呤衍生物的支气管痉挛活性和腺苷受体结合。

如本文所述，1,3-二丙基黄嘌呤的醛衍生物构成了一系列新的选择性腺苷配体，显示出支气管痉挛活性。还考虑了 8-苯基黄嘌呤的第 3 位和第 4 位取代的影响。合成的化合物在不同的腺苷受体亚型（A1、A2A、A2B 和 A3）上显示出不同的结合亲和力，并且对组胺气溶胶诱发的豚鼠哮喘具有良好的体内支气管痉挛活性。大多数化合物对 A2A 受体亚型显示出最大的亲和力。发现具有二乙基部分的单取代 3-氨基烷氧基 8-苯基黄嘌呤（化合物 12e）是最有效的 A2A 腺苷受体配体（Ki = 0.036 µM），其次是二取代的 4-氨基烷氧基-3-甲氧基-8-苯基黄嘌呤（Ki = 0.