Colotta V, Catarzi D, Varano F, Melani F, Filacchioni G, Cecchi L, Trincavelli L, Martini C, Lucacchini A
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Florence, Italy.
Farmaco. 1998 Mar;53(3):189-96. doi: 10.1016/s0014-827x(98)00006-8.
A series of pyrano[2,3-c]pyrazol-4-ones was synthesized and evaluated for bovine brain adenosine A1 and A2A receptor binding affinity. Substituents at positions 5 and/or 6 were varied in order to define the structure-activity relationships in these new kinds of adenosine receptor ligands. The most selective and potent ligand among the reported compounds was the 1,4-dihydro-1-phenyl-3-methyl-6-(3-aminophenyl)-pyrano[2,3-c]pyraz ol-4-one 11 which showed a 27-fold selectivity for A1 receptor and a Ki value of 84 nM.
合成了一系列吡喃并[2,3 - c]吡唑 - 4 - 酮，并对其进行了牛脑腺苷A1和A2A受体结合亲和力的评估。改变5位和/或6位的取代基，以确定这些新型腺苷受体配体的构效关系。在所报道的化合物中，最具选择性和活性的配体是1,4 - 二氢 - 1 - 苯基 - 3 - 甲基 - 6 -（3 - 氨基苯基）- 吡喃并[2,3 - c]吡唑 - 4 - 酮11，它对A1受体的选择性为27倍，Ki值为84 nM。
