Hariri Elham, Mahboubi Arash, Fathi Mohammad, Rahmani Parisa, Haj Mohammad Ebrahim Tehrani Kamaleddin, Babaeian Mohammad, Mashayekhi Vida, Kobarfard Farzad
Department of Medicinal Chemistry, School of Pharmacy, Phytochemistry Research Center, Shahid Beheshti University of Medical Sciences, Iran.
Department of Pharmaceutics, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Iran.
Iran J Pharm Res. 2016 Winter;15(Suppl):29-35.
A series of hydroxyl semicarbazone derivatives of substituted diaryl ketones and acetophenones were synthesized and their structures were confirmed by analytical and spectroscopic methods including elemental analysis, infrared and nuclear magnetic resonance spectroscopy. The derivatives were prepared by a condensation reaction between -hydroxy semicarbazide and substituted diaryl ketones or acetophenones leading to the desired hydroxysemicarbazones with excellent purity. The synthesized hydrazones were then evaluated for their inhibitory activity against bacterial strains including , , , and . Among the tested derivatives, compounds 2, 6 and 7 exhibited the highest bioactivity. Analysis of the activity data suggests that hydrophilicity is an important factor for the bioactivity of compounds 2 and 6 and also their selectivity over the gram-negative bacteria.
合成了一系列取代二芳基酮和苯乙酮的羟基氨基脲衍生物，并通过元素分析、红外光谱和核磁共振光谱等分析和光谱方法对其结构进行了确证。这些衍生物是通过羟基氨基脲与取代二芳基酮或苯乙酮之间的缩合反应制备的，得到了纯度优异的所需羟基氨基脲。然后评估了合成的腙对包括、、、和在内的细菌菌株的抑制活性。在测试的衍生物中，化合物2、6和7表现出最高的生物活性。活性数据分析表明，亲水性是化合物2和6生物活性及其对革兰氏阴性菌选择性的重要因素。
