STUDIES ON 6α-SUBSTITUTED PENICILLINS
II. SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF 6β-(2-ARYL-2-SULFOACETAMIDO)-6α-METHOXY PENICILLANIC ACIDS
1986 年 39 巻 10 号 p. 1419-1429
詳細
1986 年 39 巻 10 号 p. 1419-1429
The synthesis and antibacterial activity of 6α-methoxysulbenicillin analogues (2) are described. Structure-activity studies of these derivatives bearing hydrophilic substituents in the phenyl ring led to the identification of disodium 6β-[D-2-(3, 4-dihydroxyphenyl)-2-sulfoacetamido]-6α-methoxypenicillanate (2m) as a compound with potent activity against Pseudomonas aeruginosa including β-lactamase producing strains. Additional substitution of 2m gave derivatives 2p, 2q, 2r, with a further improvement in activity against Gram-negative bacteria.
