In vitro evaluation of BO-3482, a novel dithiocarbamate carbapenem with activity against methicillin-resistant staphylococci
In vitro evaluation of BO-3482, a novel dithiocarbamate carbapenem with activity against methicillin-resistant staphylococci
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DOI：
10.1128/aac.41.10.2282
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发表时间：
1997-10-01
影响因子：
4.9
通讯作者：
Nakagawa, S
中科院分区：
文献类型：
--
作者：
Adachi, Y;Nakamura, K;Nakagawa, S
BO-3482是一种二硫代氨基甲酸酯碳青霉烯，在6.25 μ g/ml时抑制耐甲氧西林葡萄球菌（MRS）的临床分离株（90%的测试分离株被抑制的MIC [MIC 90]），而亚胺培南的MIC 90>100 μ g/ml。BO-3482对甲氧西林敏感的金黄色葡萄球菌、链球菌、肠球菌和革兰氏阴性菌的活性通常低于亚胺培南，但BO-3482对屎肠球菌、流感嗜血杆菌、奇异变形杆菌和艰难梭菌的活性（MIC 90）优于亚胺培南。BO-3482对MRS的青霉素结合蛋白（PBP）PBP 2 ′和屎肠球菌的PBP 5（两种PBP对普通β-内酰胺抗生素具有低亲和力）的亲和力（50%抑制浓度）分别为3.8和20 μ g/ml，反映BO-3482对MRS的活性大于对屎肠球菌的活性。屎室
BO-3482, a dithiocarbamate carbapenem, inhibited clinical isolates of methicillin-resistant staphylococci (MRS) at 6.25 mu g/ml (MIC at which 90% of isolates tested are inhibited [MIC90]), while the MIC90 of imipenem was >100 mu g/ml. BO-3482 was generally less active than imipenem against methicillin-susceptible Staphylococcus aureus, streptococci, enterococci, and gram-negative bacteria, although BO-3482 showed better activity (MIC90) than imipenem against Enterococcus faecium, Haemophilus influenzae, Proteus mirabilis, and Clostridium difficile. The affinities (50% inhibitory concentrations) of BO-3482 for penicillin-binding protein (PBP) PBP 2' of MRS and PBP 5 of E.faecium (both PBPs have low affinities for ordinary beta-lactam antibiotics) were 3.8 and 20 mu g/ml, respectively, reflecting the greater activity of BO-3482 against MRS than against E. faecium.