Related Experiment Video
Updated: May 12, 2026

Assay Development for High-Throughput Drug Screening Against Mycobacteria
Published on: October 25, 2024
Novel semisynthetic antibiotics from caprazamycins A-G: caprazene derivatives and their antibacterial activity
Yoshiaki Takahashi1, Masayuki Igarashi, Toshiaki Miyake
1Institute of Microbial Chemistry (BIKAKEN), Kawasaki, Kanagawa, Japan. takashow@bikaken.or.jp
Abstract:
Acidic treatment of a mixture of caprazamycins (CPZs) A-G isolated from a screen of novel antimycobacterial agents gave caprazene, a core structure of CPZs, in high yield. Chemical modification of the resulting caprazene was performed to give its various derivatives. The structure-activity relationships of the caprazene derivatives against several mycobacterial species and pathogenic Gram-positive and Gram-negative bacteria were studied. Although caprazene showed no antibacterial activity, the antibacterial activity was restored for its 1'''-alkylamide, 1'''-anilide and 1'''-ester derivatives. Compounds 4b (CPZEN-45), 4d (CPZEN-48), 4f and 4g (CPZEN-51) exhibited more potent activities against Mycobacterium tuberculosis and M. avium complex strains than CPZ-B. These results suggest that caprazene would be a good precursor from which novel semisynthetic antibacterial antibiotics can be designed for the treatment of mycobacterial diseases such as tuberculosis and M. avium complex infection.
Related Concept Videos
Inhibitors of Gram-positive Cell Wall Synthesis
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
Gene Regulation in Microbial Communities: Quorum Sensing
Antifungal Agents
Antimicrobial Effectiveness
Combined Effects of Drugs: Synergism
Such synergistic combinations...

