与泰乐菌素相关的16元大环内酯类抗生素3,4''-酯衍生物的制备与评价

Preparation and evaluation of 3,4''-ester derivatives of 16-membered macrolide antibiotics related to tylosin.

作者信息

Kirst H A, Debono M, Willard K E, Truedell B A, Toth J E, Turner J R, Berry D R, Briggs B B, Fukuda D S, Daupert V M

出版信息

J Antibiot (Tokyo). 1986 Dec;39(12):1724-35. doi: 10.7164/antibiotics.39.1724.

DOI:10.7164/antibiotics.39.1724

Abstract

A large group of ester derivatives of tylosin-related macrolides was prepared in which the hydroxyl groups at C-3 and C-4'' were acylated by either chemical or biochemical methods. Most of the derivatives exhibited excellent in vitro antimicrobial activity. However, only the 3,4''-diacyl derivatives of tylosin and macrocin showed any significant improvements of in vivo efficacy against experimental infections in rodents.

摘要

制备了一大类泰乐菌素相关大环内酯的酯衍生物，其中C-3和C-4''位的羟基通过化学或生化方法进行了酰化。大多数衍生物表现出优异的体外抗菌活性。然而，只有泰乐菌素和大菌素的3,4''-二酰基衍生物在针对啮齿动物实验性感染的体内疗效上有任何显著改善。