The discovery and optimisation of a new class of benzothiazole small molecules that inhibit bacterial DNA gyrase and topoisomerase IV are described. Antibacterial properties have been demonstrated by activity against DNA gyrase ATPase and potent activity against Staphylococcus aureus, Enterococcus faecalis, Streptococcus pyogenes and Haemophilus influenzae. Further refinements to the scaffold designed
描述和优化抑制细菌DNA促旋酶和拓扑异构酶IV的新型
苯并噻唑小分子的发现和优化。对DNA促旋酶
ATPase的活性和对
金黄色葡萄球菌,粪肠球菌,化脓性链球菌和流感嗜血杆菌的活性证明了抗菌性能。设计用于增强药物相似性的支架的进一步改进包括带有
羧酸基团的α-取代基的类似物,从而产生出色的溶解性和良好的药代动力学特性。