泰乐菌素的10,11,12,13-四氢衍生物。II. 4'-脱氧-10,11,12,13-四氢去碳霉糖泰乐菌素的合成、抗菌活性及组织分布

10,11,12,13-Tetrahydro derivatives of tylosin. II. Synthesis, antibacterial activity and tissue of 4'-deoxy-10,11,12,13-tetrahydrodesmycosin.

作者信息

Narandja A, Kelneríc Z, Kolacny-Babíc L, Djokić S

机构信息

PLIVA-Pharmaceutical, Chemical, Food and Cosmetic Industry, Research Institute, Zgreb, Croatia.

出版信息

J Antibiot (Tokyo). 1995 Mar;48(3):248-53. doi: 10.7164/antibiotics.48.248.

DOI:10.7164/antibiotics.48.248

PMID:7730160

Abstract

4'-Deoxy-10,11,12,13-tetrahydrodesmycosin was prepared in six-step reactions. Antibacterial screening shows retained antibacterial spectrum of tylosin with some improvement against tylosin-sensitive Staphylococci and Haemophilus influenze. However, the pharmacokinetic data demonstrated rapid distribution from blood in tissues and prolonged maintenance in all tissues, especially in the lungs, in comparison with tylosin.

摘要

4'-脱氧-10,11,12,13-四氢泰乐菌素通过六步反应制备而成。抗菌筛选表明，它保留了泰乐菌素的抗菌谱，对泰乐菌素敏感的葡萄球菌和流感嗜血杆菌的抗菌活性有所提高。然而，与泰乐菌素相比，其药代动力学数据显示，它在组织中的血药分布迅速，且在所有组织中，尤其是肺部，维持时间延长。