Curti C, Laget M, Carle A Ortiz, Gellis A, Vanelle P
Laboratoire de Chimie Organique Pharmaceutique, Université de la Méditerranée, UMR CNRS 6517, Faculté de Pharmacie, 27 boulevard Jean Moulin, 13385 Marseille Cedex 05, France.
Eur J Med Chem. 2007 Jun;42(6):880-4. doi: 10.1016/j.ejmech.2006.12.015. Epub 2007 Jan 9.
An original one-pot microwave reaction was developed for the synthesis of sulfone derivatives as new potent antimicrobial agents. This eco-friendly methodology conducted in 30min led to desired products with good yields. The sulfones (4a and 4b) were obtained via the reaction of 3a with the corresponding halo-derivatives in the presence of sodium hydride. All compounds were tested for their antibacterial and antifungal activities against four bacterial strains (two gram positive, and two gram negative ones) and two yeasts. The disk diffusion method has shown an interesting antibacterial activity for seven compounds (3b-g and 4b) against Staphylococcus aureus. Among these seven compounds, five derivatives (3b-e and 3g) showed activity against Candida tropicalis.
开发了一种用于合成作为新型强效抗菌剂的砜衍生物的原创一锅法微波反应。这种在30分钟内进行的环保方法能以良好的产率得到所需产物。砜类化合物(4a和4b)是通过3a与相应的卤代衍生物在氢化钠存在下反应制得的。对所有化合物针对四种细菌菌株(两种革兰氏阳性菌和两种革兰氏阴性菌)以及两种酵母菌进行了抗菌和抗真菌活性测试。纸片扩散法显示七种化合物(3b - g和4b)对金黄色葡萄球菌具有有趣的抗菌活性。在这七种化合物中,五种衍生物(3b - e和3g)对热带假丝酵母菌有活性。