Ueo K, Fukuoka Y, Hayashi T, Yasuda T, Taki H, Tai M, Watanabe Y, Saikawa I, Mitsuhashi S
Antimicrob Agents Chemother. 1977 Oct;12(4):455-60. doi: 10.1128/AAC.12.4.455.
T-1220, sodium 6-[d-(-)-alpha-(4-ethyl-2,3-dioxo-1-piperazinylcarbonyl-amino)- alpha-phenylacetamido] penicillanate, is a new semisynthetic penicillin derivative that possesses a broad spectrum of in vitro antibacterial activity against gram-positive and gram-negative bacteria. T-1220 is more effective than carbenicillin (CB-PC) against Pseudomonas aeruginosa, Klebsiella pneumoniae, Proteus species, and Serratia marcescens. Addition of human serum to culture media did not significantly alter the antibacterial activity of T-1220. Greater bactericidal activity toward various strains of gram-negative bacteria was demonstrated with T-1220 than with CB-PC. T-1220, like penicillin G, was hydrolyzed by penicillinase, but was sable to a type IV penicillinase produced by P. aeruginosa strains. In vivo antibacterial activities of T-1220, ampicillin (AB-PC), and CB-PC were compared, using systemic infections of mice with P. aeruginosa, K. pneumoniae, and Escherichia coli. The 50% effective doses (milligrams per kilogram) of T-1220 were consistently lower than those of AB-PC and CB-PC.
T - 1220，即6 - [d - (-)-α-(4 - 乙基 - 2,3 - 二氧代 - 1 - 哌嗪基羰基 - 氨基)-α - 苯乙酰胺基]青霉烷酸钠，是一种新型半合成青霉素衍生物，对革兰氏阳性菌和革兰氏阴性菌具有广泛的体外抗菌活性。T - 1220对铜绿假单胞菌、肺炎克雷伯菌、变形杆菌属和粘质沙雷氏菌的抗菌活性比羧苄青霉素（CB - PC）更强。向培养基中添加人血清不会显著改变T - 1220的抗菌活性。与CB - PC相比，T - 1220对各种革兰氏阴性菌菌株表现出更强的杀菌活性。与青霉素G一样，T - 1220可被青霉素酶水解，但对铜绿假单胞菌菌株产生的IV型青霉素酶具有耐受性。利用小鼠全身性感染铜绿假单胞菌、肺炎克雷伯菌和大肠杆菌，比较了T - 1220、氨苄青霉素（AB - PC）和CB - PC的体内抗菌活性。T - 1220的50%有效剂量（毫克/千克）始终低于AB - PC和CB - PC。
