Yoshioka T, Kiyoshima K, Maeda M, Sakamoto M, Ishikura T, Fukagawa Y, Sawa T, Hamada M, Naganawa H, Takeuchi T
Sanraku Inc., Central Research Laboratories, Fujisawa, Japan.
J Antibiot (Tokyo). 1988 Nov;41(11):1617-28. doi: 10.7164/antibiotics.41.1617.
Eleven 4''-O-acyltylosin derivatives were synthesized and subjected to a two-step screening system consisting of antimicrobial activity and esterase stability assays. The new derivatives were all active against macrolide-resistant Staphylococci and mycoplasmas, but only 4''-O-(4-methoxy)phenylacetyltylosin and 4''-O-(4-acetyl)phenylacetyltylosin showed better resistance to mouse liver esterase than 4''-O-phenylacetyltylosin (reference compound C).
合成了11种4''-O-酰基泰乐菌素衍生物，并对其进行了由抗菌活性和酯酶稳定性测定组成的两步筛选系统测试。新衍生物对耐大环内酯类葡萄球菌和支原体均有活性，但只有4''-O-(4-甲氧基)苯乙酰泰乐菌素和4''-O-(4-乙酰基)苯乙酰泰乐菌素对小鼠肝脏酯酶的抗性比4''-O-苯乙酰泰乐菌素（参比化合物C）更好。
