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苯并[1,2 - d;3,4 - d']二咪唑和1H - 吡唑并[4,3 - b]吡啶作为假定A2A受体拮抗剂的合成。

Synthesis of benzo[1,2-d;3,4-d']diimidazole and 1H-pyrazolo[4,3-b]pyridine as putative A2A receptor antagonists.

作者信息

Piersanti Giovanni, Giorgi Luca, Bartoccini Francesca, Tarzia Giorgio, Minetti Patrizia, Gallo Grazia, Giorgi Fabrizio, Castorina Massimo, Ghirardi Orlando, Carminati Paolo

机构信息

Institute of Medicinal Chemistry, University of Urbino "Carlo Bo", Piazza del Rinascimento 6, 61029 Urbino PU, Italy.

出版信息

Org Biomol Chem. 2007 Aug 21;5(16):2567-71. doi: 10.1039/b707599e.

Abstract

The synthesis and the binding affinity for the putative adenosine receptor antagonist 6-methyl-7-[1,2,3]triazol-2-yl-1,6-dihydrobenzo[1,2-d;3,4-d']diimidazole (10) and 5-oxazol-2-yl-1H-pyrazolo[4,3-b]pyridin-3-ylamine (16) are reported. The title compounds were prepared from commercially available 1-chloro-2,4-dinitrobenzene (1) and 2-chloro-6-methoxy-3nitropyridine (11), respectively, but proved devoid of affinity for the adenosine A1 and A2A receptors.

摘要

报道了推定的腺苷受体拮抗剂6-甲基-7-[1,2,3]三唑-2-基-1,6-二氢苯并[1,2-d;3,4-d']二咪唑(10)和5-恶唑-2-基-1H-吡唑并[4,3-b]吡啶-3-基胺(16)的合成及其结合亲和力。标题化合物分别由市售的1-氯-2,4-二硝基苯(1)和2-氯-6-甲氧基-3-硝基吡啶(11)制备,但结果表明它们对腺苷A1和A2A受体没有亲和力。

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