Ungureanu M, Mangalagiu I, Grosu G, Petrovanu M
Université de Médecine et Pharmacie Jassy, Iaşi, Romania.
Ann Pharm Fr. 1997;55(2):69-72.
Continuing the investigations concerning synthesis-structure-biological activity in the pyridazine series, the results of the antimicrobial and antifungal tests of some new pyridazinium compounds are presented. The test was performed using the diffusimetric method with rustles steel cylinders based on the diffusion of the tested substances on the gelose surface. The comparative analysis of the obtained data leads to the following conclusions concerning the relation between structure and activity in the pyridazine series: 1. The cis-isomers are always more active comparatively with similar trans- isomers: 2. In the pyrrolopyridazine series we remark that the saturated or partial saturated compounds have always a stronger activity as the related aromatics derivatives. We also noticed that the saturated, partial saturated and aromatic compounds have different selectivity. Thus, the saturated are more active on the Pseudomonas aeruginosa and Candida albicans, the partial saturated are more active on the Staphylococcus aureus and Bacillus subtilis while the aromatic compounds are active on the Bacillus subtilis. 3. The influence of the Y-substitutes of para position of benzoylic radical and the substitutes of pyrrolo ring is not decisive towards activity, these affecting especially the selectivity.
继续关于哒嗪系列中合成-结构-生物活性的研究，本文展示了一些新型哒嗪鎓化合物的抗菌和抗真菌测试结果。该测试采用基于受试物质在琼脂表面扩散的带有不锈钢圆柱体的扩散法进行。对所得数据的比较分析得出了关于哒嗪系列中结构与活性关系的以下结论：1. 顺式异构体相对于类似的反式异构体总是更具活性：2. 在吡咯并哒嗪系列中，我们注意到饱和或部分饱和的化合物相对于相关的芳香族衍生物总是具有更强的活性。我们还注意到饱和、部分饱和和芳香族化合物具有不同的选择性。因此，饱和化合物对铜绿假单胞菌和白色念珠菌更具活性，部分饱和化合物对金黄色葡萄球菌和枯草芽孢杆菌更具活性，而芳香族化合物对枯草芽孢杆菌具有活性。3. 苯甲酰基对位的Y-取代基和吡咯环的取代基对活性的影响不具有决定性，这些主要影响选择性。
