A series of (Z)-2-alkyloxyimino-2-(2-aminothiazol-4-yl)acetamidopenicillins has been prepared. New methodology has been developed to prepare tertiary alkyl oximes. High stability to β-lactamases and potent antibacterial activity have been achieved against Gram-positive and certain Gram-negative organisms. Activity against methicillin-resistant Staphylococcus aureus was an unexpected finding. The cyclopentyl
已经制备了一系列的(Z)-2-烷氧基亚
氨基-2-(
2-氨基噻唑-4-基)乙酰
氨基
青霉素。已经开发出用于制备叔烷基
肟的新方法。对于革兰氏阳性和某些革兰氏阴性
生物,已经实现了对β-内酰胺酶的高度稳定性和有效的抗菌活性。对耐
甲氧西林的
金黄色葡萄球菌的活性是一个出乎意料的发现。选择了环戊基类似物4f(BRL 44154)进行进一步研究。