Colotta V, Cecchi L, Melani F, Catarzi D, Filacchioni G, Martini C, Giannaccini G, Tonelli M, Lucacchini A
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.
Drug Des Discov. 1992 Jul;8(4):325-39.
The synthesis and the benzodiazepine binding activity of some 3-methyl- and 3-phenylpyrazolo[4,5-c]quinolin-4-ones bearing a heterocyclic or a substituent which is different from an aryl moiety at position-1 are reported. Molecular modelling is used to correlate the binding affinity to the chemical features and to justify the reduced receptor affinities of the reported compounds with respect to that of CGS 8216 which is taken as the lead compound.
报道了一些在1位带有杂环或不同于芳基部分的取代基的3-甲基和3-苯基吡唑并[4,5-c]喹啉-4-酮的合成及其苯二氮䓬结合活性。利用分子建模将结合亲和力与化学特征相关联，并解释所报道化合物相对于作为先导化合物的CGS 8216而言受体亲和力降低的原因。
