Thiault G A, Le Guen Y, Boucherle A, Walrant P
Farmaco Sci. 1984 Sep;39(9):765-80.
In order to increase the pharmacological activities of the molecules described in the first part of the paper, an acetic or a 2-propionic group was introduced in to the fundamental structure, either on the aromatic ring, on the pyrrole nitrogen or on carbon 3 of the heterocycle. Moreover, a 4-chlorobenzoyl group was fixed on carbon 3 of the pyrrole via condensation of 4-chloroaniline with 4-chlorobenzoyl triketones. The structure of the adducts was demonstrated both by N.M.R. spectra and by using another unambiguous synthetic route. Finally, derivatives with the salicylic substructure on the nitrogen of the pyrrole are described. Their analgesic and anti-inflammatory properties are reported as well as some effects on the central nervous system.
为了增强论文第一部分所述分子的药理活性，在基本结构的芳环、吡咯氮原子或杂环的3位碳原子上引入了乙酰基或2-丙酰基。此外，通过4-氯苯胺与4-氯苯甲酰三酮缩合，将4-氯苯甲酰基固定在吡咯的3位碳原子上。加合物的结构通过核磁共振光谱以及另一条明确的合成路线得以证实。最后，描述了吡咯氮原子上带有水杨酸亚结构的衍生物。报告了它们的镇痛和抗炎特性以及对中枢神经系统的一些作用。
