Fundacao Oswaldo Cruz, Instituto de Tecnologia em Farmacos - Farmanguinhos. Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro, 21041-250, RJ, Brazil.
Med Chem. 2014 May;10(3):271-6. doi: 10.2174/1573406410666140218103022.
Thioetherhydroxyethylsulfonamide derivatives were synthesized and evaluated for their in vitro antibacterial activity against Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853) and Staphylococcus aureus (ATCC 25923). Results have shown that compounds 8c and 9e display potent activity (MIC = 0.125 µg/mL) against E. coli when compared with the standard drug sulfamethoxazole (SMZ, MIC < 0.5 µg/mL) for this same strain. All the new compounds were fully identified and characterized by NMR ((1)H and (13)C) and X-ray crystallography (for compound 8c). This class of compounds can be considered as a good starting point for the development of new lead molecules in the fight against multi-drug bacterial resistance.
硫醚羟乙基磺酰胺衍生物被合成并评估其对大肠杆菌（ATCC 25922）、铜绿假单胞菌（ATCC 27853）和金黄色葡萄球菌（ATCC 25923）的体外抗菌活性。结果表明，与标准药物磺胺甲恶唑（SMZ，MIC < 0.5 µg/mL）相比，化合物 8c 和 9e 对大肠杆菌具有很强的活性（MIC = 0.125 µg/mL）。所有新化合物均通过 NMR ((1)H 和 (13)C)和 X 射线晶体学（化合物 8c）进行了充分的鉴定和表征。该类化合物可被视为开发用于对抗多药耐药细菌的新型先导分子的良好起点。
