Colotta V, Cecchi L, Melani F, Filacchioni G, Martini C, Gelli S, Lucacchini A
Dipartimento di Scienze Farmaceutiche, Universita di Firenze.
J Pharm Sci. 1991 Mar;80(3):276-9. doi: 10.1002/jps.2600800317.
The synthesis of a series of 8-substituted 1,4-dihydro-1-aryl-3-methyl-[1]benzopyrano[3,4-d]pyrazol-4-ones (series 7) 2,4-dihydro-2-aryl-3-methyl[1]benzopyrano[4,3-c]pyrazol-4-ones (series 8) is reported. Compounds of series 7 and 8 were tested for their ability to displace [3H]flunitrazepam from bovine brain membranes and for their in vitro biological activity. The results allowed some conclusions to be drawn about the structural requirements of the benzodiazepine recognition site within this class of unusual ligands.
报道了一系列8-取代的1,4-二氢-1-芳基-3-甲基-[1]苯并吡喃并[3,4-d]吡唑-4-酮（系列7）和2,4-二氢-2-芳基-3-甲基[1]苯并吡喃并[4,3-c]吡唑-4-酮（系列8）的合成。测试了系列7和8化合物从牛脑膜置换[3H]氟硝西泮的能力及其体外生物活性。结果得出了关于这类特殊配体中苯二氮䓬识别位点结构要求的一些结论。
