具有强效抗耐甲氧西林金黄色葡萄球菌（MRSA）活性的2-（萘磺酰胺基）甲基碳青霉烯类的合成与性质：L-786,392的发现
Synthesis and properties of 2-(naphthosultamyl)methyl-carbapenems with potent anti-MRSA activity: discovery of L-786,392.
作者信息
Ratcliffe R W, Wilkening R R, Wildonger K J, Waddell S T, Santorelli G M, Parker D L, Morgan J D, Blizzard T A, Hammond M L, Heck J V, Huber J, Kohler J, Dorso K L, St Rose E, Sundelof J G, May W J, Hammond G G
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., Rahway, New Jersey 07065-0900, USA.
出版信息
Bioorg Med Chem Lett. 1999 Mar 8;9(5):679-84. doi: 10.1016/s0960-894x(99)00071-2.
A series of 1beta-methyl-2-(naphthosultamyl)methyl-carbapenems bearing dicationic groups on the naphthosultamyl moiety was prepared and evaluated for activity against resistant gram-positive bacteria. Based on a combination of excellent in vitro antibacterial activity, acceptable mouse acute toxicity, and a desirable fragmentation pattern on beta-lactam ring opening, the analog 2g (L-786,392) was selected for extended evaluation.
制备了一系列在萘磺酰胺部分带有双阳离子基团的1β-甲基-2-(萘磺酰胺基)甲基碳青霉烯类化合物，并评估了其对耐药革兰氏阳性菌的活性。基于出色的体外抗菌活性、可接受的小鼠急性毒性以及β-内酰胺开环时理想的裂解模式，选择类似物2g（L-786,392）进行进一步评估。
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