Vuye A
Arzneimittelforschung. 1981;31(8):1290-5.
(6R, 7R)-7-[[Carboxy(4-hydroxyphenyl)-acetyl]amino]-7-methoxy-3[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-8-oxo-5-oxa-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylic acid (moxalactam, LY 127 935), a novel 1-oxa-beta-lactam, was proved to display similar antibacterial activity as cefotaxime against a number of beta-lactamase-producing gram-negative strains. The outstanding activity proved to be bactericidal in most cases and was only slightly influenced by variation of the inoculum size. The activity of cefotaxime and especially cefamandole on the contrary had rather a high inoculum-dependence. Moxalactam had equal stability to gram-negative beta-lactamases as has cefoxitin. Like cefotaxime and cefoxitin, the compound proved to be a potent inhibitor of cephalosporinases but not of broad spectrum beta-lactamases.
(6R,7R)-7-[[羧基(4-羟基苯基)乙酰基]氨基]-7-甲氧基-3[[(1-甲基-1H-四氮唑-5-基)硫代]甲基]-8-氧代-5-氧杂-1-氮杂双环[4,2,0]辛-2-烯-2-羧酸(莫西酰胺,LY 127935),一种新型的1-氧杂-β-内酰胺,已被证明对许多产β-内酰胺酶的革兰氏阴性菌株具有与头孢噻肟相似的抗菌活性。在大多数情况下,其出色的活性被证明是杀菌性的,并且仅受接种量变化的轻微影响。相反,头孢噻肟尤其是头孢孟多的活性具有相当高的接种量依赖性。莫西酰胺对革兰氏阴性β-内酰胺酶的稳定性与头孢西丁相同。与头孢噻肟和头孢西丁一样,该化合物被证明是头孢菌素酶的有效抑制剂,但不是广谱β-内酰胺酶的抑制剂。