Sykes R B, Bonner D P, Bush K, Georgopapadakou N H
Antimicrob Agents Chemother. 1982 Jan;21(1):85-92. doi: 10.1128/AAC.21.1.85.
Azthreonam (SQ 26,776) is a synthetic monocyclic beta-lactam antimicrobial agent belonging to the monobactam family (Sykes et al., Nature [London] 291:489-491, 1981), members of which are characterized by having the 2-oxoazetidine-1-sulfonic acid moiety. Azthreonam exhibits a high degree of stability to beta-lactamases and is specifically active against aerobic gram-negative bacteria, including Pseudomonas aeruginosa. Its activity against these organisms was in general equal or superior to that observed with the third-generation cephalosporins, cefotaxime and ceftazidime. Like penicillins and cephalosporins, azthreonam interacts with essential penicillin-binding proteins of gram-negative bacteria. Azthreonam protected mice against experimental infections produced by a range of gram-negative bacteria, exhibiting efficacy comparable to that of cefotaxime and ceftazidime.
氨曲南(SQ 26,776)是一种合成的单环β-内酰胺抗菌剂,属于单酰胺菌素家族(赛克斯等人,《自然》[伦敦]291:489 - 491,1981),该家族成员的特征是具有2-氧代氮杂环丁烷-1-磺酸部分。氨曲南对β-内酰胺酶表现出高度稳定性,并且对需氧革兰氏阴性菌具有特异性活性,包括铜绿假单胞菌。它对这些微生物的活性总体上与第三代头孢菌素头孢噻肟和头孢他啶相当或更优。与青霉素和头孢菌素一样,氨曲南与革兰氏阴性菌的必需青霉素结合蛋白相互作用。氨曲南可保护小鼠免受多种革兰氏阴性菌引起的实验性感染,其疗效与头孢噻肟和头孢他啶相当。