Kurath P, Tadanier J, Johnson P, Grampovnik D, Egan R S, Stanaszek R S, Cirovic M, Washburn W H, Leonard J E
J Antibiot (Tokyo). 1981 Jun;34(6):691-700. doi: 10.7164/antibiotics.34.691.
The preparation of 4-de-N-methylfortimicin A analogs as well as the preparation of 4-de-N-methyl-4-N-(beta-aminoethyl)-4-N-ethylfortimicin B is reported. It was shown that the 4-N-methyl group in fortimicin analogs is essential for antibacterial activity since neither the 4-de-N-methylfortimicin A nor the 4-de-N-methyl-4-N-(beta-aminoethyl)-4-N-ethylfortimicin B exhibited useful biological activity.
报道了4-去-N-甲基福提霉素A类似物的制备以及4-去-N-甲基-4-N-(β-氨基乙基)-4-N-乙基福提霉素B的制备。结果表明,福提霉素类似物中的4-N-甲基基团对抗菌活性至关重要,因为4-去-N-甲基福提霉素A和4-去-N-甲基-4-N-(β-氨基乙基)-4-N-乙基福提霉素B均未表现出有效的生物活性。