17385-88-5Relevant academic research and scientific papers
Introducing broadened antibacterial activity to rhodanine derivatives targeting enoyl-acyl carrier protein reductase
Sun, Zhi-Gang,Xu, Yun-Jie,Xu, Jian-Fei,Liu, Qi-Xing,Yang, Yu-Shun,Zhu, Hai-Liang
, p. 125 - 129 (2019)
Broadened antibacterial activity was introduced to rhodanine derivatives targeting Mycobacterial tuberculosis enoyl-acyl carrier protein reductase (Mtb InhA) by recruiting feature of xacins to bring DNA Gyrase B inhibitory capability. This is significant for preventing further bacterial injections in the tuberculosis treatment. The most potent compound Cy14 suggested comparable bioactivity (IC50=3.18μM for Mtb InhA; IC50=10nM for DNA Gyrase B) with positive controls. Structure–activity relationship discussion and molecular docking model revealed the significance of rhodanine moiety and derived methoxyl on meta-position, pointing out orientations for future modification.
