Chemical Modification of Aminoglycoside Antibiotics. Some N-Alkyl Derivatives of Sorbistin A_1 (P-2563 P) and Butirosin A

概要

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Some N-alkyl derivatives of sorbistin A_1 (P-2563 P) (1) and butirosin A (10) were prepared by reductive alkylation with aldehyde and NaBH_4 or NaBH_3CN. Among them, 4'-N-propylsorbistin A_1 (8b) showed antimicrobial activity against gram-positive bacteria comparable to sorbistin A_1 (1) and showed broader spectrum of activity against gramnegative bacteria including some of the sorbistin A_1-resistant strains (K. pneumoniae, Ps. aeruginosa) than sorbistin A_1 (1). 2'-N-Propylbutirosin A (14c) showed antimicrobial activity similar to butirosin A (10) and showed weak antimicrobial activity against some of butirosin A-resistant bacteria including E. coli JR 66/W 677 which is reported to produce 3'-phosphotransferase II. It was shown that 2'-N-propylbutirosin A (14c) was hardly phosphorylated under the condition where butirosin A (10) was almost completely phosphorylated with the purified E. coli JR 66/W 677 3'-phosphotransferase II.
公益社団法人日本薬学会の論文
1979-01-25