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三环杂芳族体系。某些1-芳基-1,4-二氢-3-甲基[1]苯并吡喃并[2,3-c]吡唑-4-酮、1-芳基-4,9-二氢-3-甲基-1H-吡唑并[3,4-b]喹啉-4-酮和1-芳基-1H-咪唑并[4,5-b]喹喔啉的合成及其对A1和A2a腺苷的结合活性

Tricyclic heteroaromatic systems. Synthesis and A1 and A2a adenosine binding activities of some 1-aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c] pyrazol-4-ones, 1-aryl-4,9-dihydro-3-methyl-1H-pyrazolo[3,4-b]quinolin-4- ones, and 1-aryl-1H-imidazo[4,5-b]quinoxalines.

作者信息

Catarzi D, Cecchi L, Colotta V, Filacchioni G, Martini C, Tacchi P, Lucacchini A

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.

出版信息

J Med Chem. 1995 Apr 14;38(8):1330-6. doi: 10.1021/jm00008a011.

DOI:10.1021/jm00008a011
PMID:7731018
Abstract

The syntheses and A1 and A2a adenosine binding activities of some new 1-aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c]pyrazol-4-ones, 1-aryl-4,9-dihydro-3-methyl-1H-pyrazolo[3,4-b]-quinolin-4-ones, and 1-aryl-1H-imidazo[4,5-b]quinoxalines are reported. Some compounds show A1 adenosine receptor affinity and selectivity. Structure-activity relationships on these new classes of adenosine receptor ligands are defined.

摘要

报道了一些新型1-芳基-1,4-二氢-3-甲基[1]苯并吡喃并[2,3-c]吡唑-4-酮、1-芳基-4,9-二氢-3-甲基-1H-吡唑并[3,4-b]喹啉-4-酮和1-芳基-1H-咪唑并[4,5-b]喹喔啉的合成及其对A1和A2a腺苷的结合活性。一些化合物表现出对A1腺苷受体的亲和力和选择性。确定了这些新型腺苷受体配体的构效关系。

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