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对新型β-内酰胺抗生素莫拉西林(LY127935)进行的体外研究,该抗生素对革兰氏阴性菌具有显著活性。

In vitro studies of moxalactam (LY127935), a new beta-lactam antibiotic with significant activity against gram-negative bacteria.

作者信息

DeMaria A, Alvarez S, Klein J O, McCabe W R

出版信息

Infection. 1980;8 Suppl 3:S 261-7. doi: 10.1007/BF01639592.

Abstract

Moxalactam (LY127935) is a new beta-lactam antibiotic which is chemically related to the cephalosporins. The agent is highly active against the Enterobacteriaceae, with most organisms sensitive to 0.1 mcg/ml or less. It is also active at low concentration against gentamicin-resistant strains of Providencia and Serratia. Minimal inhibitory concentrations of moxalactam for Pseudomonas aeruginosa are approximately four-fold lower than those of carbenicillin for the same isolates. It is highly active against Hemophilus influenzae, including ampicillin-resistant strains, with all strains tested sensitive to 0.1 mcg/ml or less. The majority of strains of Neisseria gonorrheae and Neisseria meningitidis are sensitive to 0.1 mcg/ml or less. Moxalactam is more active against Bacteroides fragilis than cefoxitin. However, activity of moxalactam against gram-positive cocci was uniformly less than cephalothin and other cephalosporins tested. Little effect of inoculum size was observed with moxalactam except for particular strains of gram-negative bacilli. The drug was found to be 40-43% bound to human serum proteins.

摘要

羟羧氧酰胺菌素(LY127935)是一种新型β-内酰胺抗生素,在化学结构上与头孢菌素相关。该药物对肠杆菌科细菌具有高度活性,大多数菌株对0.1微克/毫升或更低浓度敏感。它对普罗威登斯菌属和沙雷菌属的庆大霉素耐药菌株在低浓度时也有活性。对于相同的铜绿假单胞菌分离株,羟羧氧酰胺菌素的最低抑菌浓度比羧苄西林低约四倍。它对流感嗜血杆菌具有高度活性,包括对氨苄西林耐药的菌株,所有测试菌株对0.1微克/毫升或更低浓度敏感。大多数淋病奈瑟菌和脑膜炎奈瑟菌菌株对0.1微克/毫升或更低浓度敏感。羟羧氧酰胺菌素对脆弱拟杆菌的活性比头孢西丁更强。然而,羟羧氧酰胺菌素对革兰氏阳性球菌的活性始终低于头孢噻吩和其他测试的头孢菌素。除了特定的革兰氏阴性杆菌菌株外,未观察到接种量大小对羟羧氧酰胺菌素有显著影响。发现该药物与人类血清蛋白的结合率为40 - 43%。

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