Dipartimento di Scienze e Tecnologie Molecolari e Biomolecolari-Sezione di Chimica e Tecnologie Farmaceutiche, Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy.
Eur J Med Chem. 2012 Aug;54:709-20. doi: 10.1016/j.ejmech.2012.06.028. Epub 2012 Jun 28.
A series of isochromeno[4,3-c]pyrazole-5(1H)-one derivatives 7b-h were prepared and tested at 10 μM for their ability to displace specific [(3)H]flunitrazepam from bovine brain membranes. The substitution pattern of the above derivatives was shown to influence the receptor affinity. The most active compound of the series was 7e, showing a 54% inhibition of [(3)H]flunitrazepam binding. Compounds 7a-d,i were compared with the known isomers chromeno[4,3-c]pyrazole-4(1H)-ones 14a-d,i, showing that the isochromene/chromene isomerism influences the activity.
一系列异噁唑并[4,3-c]吡唑-5(1H)-酮衍生物 7b-h 被制备出来，并在 10 μM 浓度下进行了测试，以评估它们取代牛脑膜中特定 [(3)H]氟硝西泮的能力。上述衍生物的取代模式被证明会影响受体亲和力。该系列中最活跃的化合物是 7e，其对 [(3)H]氟硝西泮结合的抑制率为 54%。化合物 7a-d,i 与已知的异构体色烯并[4,3-c]吡唑-4(1H)-酮 14a-d,i 进行了比较，结果表明异噁唑并/色烯的异构化会影响活性。
