Nishimura S, Sasaki H, Yasuda N, Matsumoto Y, Kamimura T, Sakane K, Takaya T
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.
J Antibiot (Tokyo). 1989 Jul;42(7):1124-32. doi: 10.7164/antibiotics.42.1124.
A series of 7 alpha-hydroxyethyl-1-oxacephems (1) was synthesized. The main focus of this study was to investigate biological activity relationships between 1-oxacephems (1) and the corresponding cephems (2). Replacement of the sulfur atom of 2 by the oxygen atom caused an enhancement of antibacterial activity, although the antibacterial activity of 1 was not high enough. Additionally 1 showed beta-lactamase inhibitory activity, especially against cephalosporinase. However, the potency was lower than that of 2.
合成了一系列7-α-羟乙基-1-氧杂头孢烯（1）。本研究的主要重点是研究1-氧杂头孢烯（1）与相应头孢烯（2）之间的生物活性关系。用氧原子取代2中的硫原子导致抗菌活性增强，尽管1的抗菌活性不够高。此外，1表现出β-内酰胺酶抑制活性，尤其是对头孢菌素酶。然而，其效力低于2。
