一系列含有C(3)-甲基氨基吡啶硫甲基取代基的C(7)-取代氧亚氨基头孢菌素的构效关系。BRL 57342及一些类似物的合成与生物学特性
Structure-activity relationships within a series of C(7)-substitutedoxyiminocephalosporins containing the C(3)-methylaminopyridiniumthiomethyl substituent. Synthesis and biological properties of BRL 57342 and some close analogues.
作者信息
Adams R G, Brain E G, Branch C L, Guest A W, Harrington F P, Mizen L, Neale J E, Pearson M J, Simpson I N, Smulders H
机构信息
SmithKline Beecham Pharmaceuticals, Research Division, Betchworth, Surrey, U.K.
出版信息
J Antibiot (Tokyo). 1995 May;48(5):417-24. doi: 10.7164/antibiotics.48.417.
(6R,7R)-7-[2-(2-Amino-4-thiazolyl)-2-[(Z)-[(S)-carboxy(3,4- dihydroxyphenyl)methyl]oxyimino]acetamido]-3-(1-methylaminopyri dinium-4-thiomethyl)ceph-3-em-4-carboxylate sodium salt (BRL 57342, 1f) combines excellent in vitro antibacterial potency against Gram-positive and Gram-negative bacteria, including P. aeruginosa and Acinetobacter spp., with excellent stability to extended spectrum beta-lactamases. This potency is reflected in in vivo efficacy studies.
（6R，7R）-7-[2-（2-氨基-4-噻唑基）-2-[(Z)-[(S)-羧基（3,4-二羟基苯基）甲基]氧亚氨基]乙酰胺基]-3-（1-甲基氨基吡啶-4-硫甲基）头孢-3-烯-4-羧酸钠盐（BRL 57342，1f）对革兰氏阳性菌和革兰氏阴性菌，包括铜绿假单胞菌和不动杆菌属，具有优异的体外抗菌效力，并且对超广谱β-内酰胺酶具有出色的稳定性。这种效力在体内疗效研究中得到了体现。
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