Dipartimento di Scienze Farmaceutiche, Università di Milano, Via Mangiagalli 25, I-20133 Milano, Italy.
Department of Medical Biothechnologies and Translational Medicine, Università di Milano, Via Vanvitelli 32, I-20129 Milano, Italy.
Eur J Med Chem. 2015 Jan 7;89:252-65. doi: 10.1016/j.ejmech.2014.09.100. Epub 2014 Oct 18.
A SAR study was performed on 3-substituted 2,6-difluorobenzamides, known inhibitors of the essential bacterial cell division protein FtsZ, through a series of modifications first of 2,6-difluoro-3-nonyloxybenzamide and then of its 3-pyridothiazolylmethoxy analogue PC190723. The study led to the identification of chiral 2,6-difluorobenzamides bearing 1,4-benzodioxane-2-methyl residue at the 3-position as potent antistaphylococcal compounds.
研究人员对已知的细菌必需蛋白 FtsZ 的抑制剂——3-取代 2,6-二氟苯甲酰胺进行了构效关系研究,通过对 2,6-二氟-3-壬氧基苯甲酰胺及其 3-吡啶并噻唑基甲氧基类似物 PC190723 进行一系列修饰,发现 3-位含有 1,4-苯并二恶烷-2-甲基取代基的手性 2,6-二氟苯甲酰胺类化合物具有较强的抗葡萄球菌活性。