Abstract
Analogs of CPZEN-45, which is expected to be a promising new antituberculosis drug that overcomes the shortcomings of caprazamycins, were synthesized and their biological activities were evaluated. The biological activity of analogs 1–3, which converted the anilide portion, and analogs 4 and 5, focusing on the seven-membered ring, were lower than that of CPZEN-45. These results suggest that the inhibitory activity of CPZEN-45 against TagO, an ortholog of WecA, has a strict structural limitation, and it was hoped for elucidation of the mode of action of CPZEN-45 using structural biology in the future.
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Acknowledgements
We are grateful to Dr. Kiyoko Iijima of the Institute of Microbial Chemistry (BIKAKEN) for assistance with the NMR spectrometry experiments.
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This article is dedicated to Dr. Kiyoshi Isono’s 88 years anniversary, and his long-standing contribution to the study of antibiotics.
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Ishizaki, Y., Takahashi, Y., Kimura, T. et al. Synthesis and biological activity of analogs of CPZEN-45, a novel antituberculosis drug. J Antibiot 72, 970–980 (2019). https://doi.org/10.1038/s41429-019-0225-5
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DOI: https://doi.org/10.1038/s41429-019-0225-5
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