Neu H C, Chin N X, Jules K, Labthavikul P
J Antimicrob Chemother. 1986 Apr;17(4):441-52. doi: 10.1093/jac/17.4.441.
The in-vitro activity of BMY 28142, an iminomethoxy, aminothiazolyl cephalosporin containing a methyl pyrrolidinio C-3 was compared with that of cefotaxime, ceftazidime, aztreonam, imipenem and tobramycin against various bacteria. BMY 28142 was the most active agent tested against the Enterobacteriaceae inhibiting 90% at less than or equal to 1 mg/l. The in-vitro activity of BMY 28142 was equal to or superior to cefotaxime against the highly susceptible members of the Enterobacteriaceae and several-fold superior to ceftazidime and aztreonam. BMY 28142 inhibited many Enterobacter cloacae, Citrobacter freundii and Serratia marcescens resistant to cefotaxime, ceftazidime and aztreonam. BMY 28142 was more active than imipenem against Proteus, Providencia and Morganella species. Ceftazidime and imipenem were more active than BMY 28142 against Pseudomonas aeruginosa, but it inhibited piperacillin and tobramycin-resistant isolates. BMY 28142 inhibited beta-lactamase producing Haemophilus influenzae and Neisseria gonorrhoeae. BMY 28142 was more active than ceftazidime against streptococcal and staphylococcal species, but it did not inhibit or kill most methicillin-resistant Staphylococcus aureus. BMY 28142 did not inhibit most Bacteroides species. BMY 28142 was not hydrolyzed by common plasmid and chromosomal beta-lactamases, but it bound poorly to Enterobacter beta-lactamase, was a poor inhibitor of the TEM plasmid beta-lactamase and was a poor inducer of beta-lactamases.
将含甲基吡咯烷鎓C-3的亚胺甲氧基氨基噻唑头孢菌素BMY 28142的体外活性与头孢噻肟、头孢他啶、氨曲南、亚胺培南及妥布霉素针对多种细菌的活性进行了比较。BMY 28142是所测试的对肠杆菌科细菌活性最强的药物,在浓度小于或等于1毫克/升时可抑制90%的该类细菌。BMY 28142对肠杆菌科中高度敏感菌的体外活性等于或优于头孢噻肟,比头孢他啶和氨曲南强几倍。BMY 28142可抑制许多对头孢噻肟、头孢他啶和氨曲南耐药的阴沟肠杆菌、弗氏柠檬酸杆菌和粘质沙雷氏菌。BMY 28142对变形杆菌属、普罗威登斯菌属和摩根菌属的活性比亚胺培南更强。头孢他啶和亚胺培南对铜绿假单胞菌的活性比BMY 28142更强,但BMY 28142可抑制对哌拉西林和妥布霉素耐药的菌株。BMY 28142可抑制产β-内酰胺酶的流感嗜血杆菌和淋病奈瑟菌。BMY 28142对链球菌属和葡萄球菌属的活性比头孢他啶更强,但不能抑制或杀灭大多数耐甲氧西林金黄色葡萄球菌。BMY 28142不能抑制大多数拟杆菌属细菌。BMY 28142不被常见的质粒和染色体β-内酰胺酶水解,但与阴沟肠杆菌β-内酰胺酶结合不佳,是TEM质粒β-内酰胺酶的弱抑制剂,也是β-内酰胺酶的弱诱导剂。