Ochiai M, Morimoto A, Matsushita Y, Kida M
J Antibiot (Tokyo). 1980 Sep;33(9):1014-21. doi: 10.7164/antibiotics.33.1014.
7 beta-[2-(2-Aminothiazol-4-yl)acetamido]-7 alpha-methoxycephalosporins were synthesized both by acylation of the 7 beta-amino-7 alpha-methoxycephalosporin compound (VIII) and a new direct acyl-exchange reaction of 7 alpha-methoxy-7 beta-phosphoramido compound (VII). Some of these compounds (IXa, IXb) showed higher antibacterial activity than the 7 alpha-unsubstituted compound against beta-lactamase-producing strains of Serratia marcescens and Proteus vulgaris.
7β-[2-(2-氨基噻唑-4-基)乙酰胺基]-7α-甲氧基头孢菌素是通过7β-氨基-7α-甲氧基头孢菌素化合物(VIII)的酰化反应以及7α-甲氧基-7β-磷酰胺化合物(VII)的一种新的直接酰基交换反应合成的。其中一些化合物(IXa、IXb)对产β-内酰胺酶的粘质沙雷氏菌和普通变形杆菌菌株显示出比7α-未取代化合物更高的抗菌活性。