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 Dec;58:64-71. doi: 10.1016/j.ejmech.2012.09.041. Epub 2012 Oct 1.
Several new 4-diazopyrazole derivatives 6a-g and 9a-c were obtained by the reaction of 1-(R-substituted-phenyl)-3-(1,3-dimethyl-1H-pyrazol-5-yl)ureas 5a-g and N-(1,3-dimethyl-1H-pyrazol-5-yl)-2-(R-substituted-phenyl)acetamides 8a-c respectively with a sevenfold excess of nitrous acid in acetic acid solution. The compounds were assayed for their activity against the Staphylococcus aureus reference strains ATCC 25923, ATCC 29213 and ATCC 6538, as well as six veterinary strains. The best anti-staphylococcal profile was showed by (R-substituted-phenyl)acetylazanides 9a,c. Compound 9c was also able at 3.1 μg mL(-1) to inhibit of 45.7% the biofilm formation of the strains S. aureus ATCC 29213.
通过 1-(R-取代苯基)-3-(1,3-二甲基-1H-吡唑-5-基)脲 5a-g 与 N-(1,3-二甲基-1H-吡唑-5-基)-2-(R-取代苯基)乙酰胺 8a-c 的反应，得到了几种新的 4-二氮杂吡唑衍生物 6a-g 和 9a-c。在乙酸溶液中，用七倍过量的亚硝酸处理这些化合物，以评估它们对金黄色葡萄球菌参考菌株 ATCC 25923、ATCC 29213 和 ATCC 6538 以及六种兽医菌株的活性。(R-取代苯基)乙酰基氮烷的抗葡萄球菌特性最好。化合物 9c 在 3.1μg mL(-1)时也能够抑制金黄色葡萄球菌 ATCC 29213 生物膜形成的 45.7%。
