Adachi Y, Nakamura K, Kato Y, Hazumi N, Hashizume T, Nakagawa S
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Japan.
Antimicrob Agents Chemother. 1997 Oct;41(10):2282-5. doi: 10.1128/AAC.41.10.2282.
BO-3482, a dithiocarbamate carbapenem, inhibited clinical isolates of methicillin-resistant staphylococci (MRS) at 6.25 microg/ml (MIC at which 90% of isolates tested are inhibited [MIC90]), while the MIC90 of imipenem was > 100 microg/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 microg/ml, respectively, reflecting the greater activity of BO-3482 against MRS than against E. faecium.
BO - 3482是一种二硫代氨基甲酸盐碳青霉烯类药物，它对耐甲氧西林葡萄球菌（MRS）临床分离株的最低抑菌浓度（MIC，即能抑制90%受试分离株生长的最低药物浓度[MIC90]）为6.25微克/毫升，而亚胺培南对这些菌株的MIC90>100微克/毫升。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，不过BO - 3482对粪肠球菌、流感嗜血杆菌、奇异变形杆菌和艰难梭菌的活性（MIC90）比亚胺培南更好。BO - 3482对MRS的青霉素结合蛋白（PBP）PBP 2'以及粪肠球菌的PBP 5（这两种PBP对普通β-内酰胺类抗生素的亲和力较低）的亲和力（50%抑制浓度）分别为3.8和20微克/毫升，这表明BO - 3482对MRS的活性高于对粪肠球菌的活性。
