Burton G, Basker M J, Bentley P H, Best D J, Dixon R A, Harrington F P, Kenyon R F, Lashford A G, Taylor A W
J Antibiot (Tokyo). 1985 Jun;38(6):721-39. doi: 10.7164/antibiotics.38.721.
The influence on the antibacterial activity of introducing a 6 alpha-methoxy group into carbenicillin, and various 6 alpha-substituents into sulbenicillin and piperacillin was examined. Further variations of the side chain aryl group were examined in the 6 alpha-methoxy substituted series. This led to the identification of disodium 6 beta-(D,L-2-carboxy-2-thien-3-ylacetamido)-6 alpha-methoxypenicillanate (5b) as a beta-lactamase stable derivative with useful activity against Enterobacteriaceae, and disodium 6 beta-[D-2-(4-aminophenyl)-2-sulfoacetamido]-6 alpha-methoxypenicillanate (6e) with slightly lower activity against the Enterobacteriaceae but more active against Pseudomonas aeruginosa.
研究了在羧苄西林中引入6α-甲氧基以及在磺苄西林和哌拉西林中引入各种6α-取代基对抗菌活性的影响。在6α-甲氧基取代系列中进一步研究了侧链芳基的变化。这导致鉴定出6β-(D,L-2-羧基-2-噻吩-3-基乙酰胺基)-6α-甲氧基青霉烷酸钠(5b)为一种对β-内酰胺酶稳定的衍生物，对肠杆菌科细菌具有有效活性，以及6β-[D-2-(4-氨基苯基)-2-磺基乙酰胺基]-6α-甲氧基青霉烷酸钠(6e)，其对肠杆菌科细菌的活性略低，但对铜绿假单胞菌更具活性。
