PREPARATION AND EVALUATION OF 3, 4"-ESTER DERIVATIVES OF 16-MEMBERED MACROLIDE ANTIBIOTICS RELATED TO TYLOSIN

H. A. KIRST; M. DEBONO; K. E. WILLARD; B. A. TRUEDELL; J. E. TOTH; J. R. TURNER; D. R. BERRY; B. B. BRIGGS; D. S. FUKUDA; V. M. DAUPERT; A. M. FELTY-DUCKWORTH; J. L. OTT; F. T. COUNTER

doi:10.7164/antibiotics.39.1724

H. A. KIRST, M. DEBONO, K. E. WILLARD, B. A. TRUEDELL, J. E. TOTH, J. R. TURNER, D. R. BERRY, B. B. BRIGGS, D. S. FUKUDA, V. M. DAUPERT, A. M. FELTY-DUCKWORTH, J. L. OTT, F. T. COUNTER

Author information

H. A. KIRST
The Lilly Research Laboratories, Eli Lilly and Company
M. DEBONO
The Lilly Research Laboratories, Eli Lilly and Company
K. E. WILLARD
The Lilly Research Laboratories, Eli Lilly and Company
B. A. TRUEDELL
The Lilly Research Laboratories, Eli Lilly and Company
J. E. TOTH
The Lilly Research Laboratories, Eli Lilly and Company
J. R. TURNER
The Lilly Research Laboratories, Eli Lilly and Company
D. R. BERRY
The Lilly Research Laboratories, Eli Lilly and Company
B. B. BRIGGS
The Lilly Research Laboratories, Eli Lilly and Company
D. S. FUKUDA
The Lilly Research Laboratories, Eli Lilly and Company
V. M. DAUPERT
The Lilly Research Laboratories, Eli Lilly and Company
A. M. FELTY-DUCKWORTH
The Lilly Research Laboratories, Eli Lilly and Company
J. L. OTT
The Lilly Research Laboratories, Eli Lilly and Company
F. T. COUNTER
The Lilly Research Laboratories, Eli Lilly and Company

JOURNALS FREE ACCESS

Volume 39 (1986) Issue 12 Pages 1724-1735

DOI https://doi.org/10.7164/antibiotics.39.1724

Details

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.

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