Citation: Zi-Jie Liu, Xiao-Yong Guo, Gang Liu. N-Oxide heterocycles and imidazoles replacing ring D of calanolides against Mycobacterium tuberculosis[J]. Chinese Chemical Letters, ;2016, 27(01): 51-54. doi: 10.1016/j.cclet.2015.11.001 shu

N-Oxide heterocycles and imidazoles replacing ring D of calanolides against Mycobacterium tuberculosis

Zi-Jie Liu ^a ,
Xiao-Yong Guo ^a ,
Gang Liu ^a,b,,

1.
a Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China;
2.
b Tsinghua-Peking Center for Life Sciences and Department of Pharmacology and Pharmaceutical Sciences, School of Medicine, Tsinghua University, Beijing 100084, China

Corresponding author: Gang Liu,
Received Date: 10 July 2015
Available Online: 6 September 2015

We have explored the chemistry of N-oxide heterocycles and imidazoles replacing ring D of the natural product(+)-calanolide A, and have synthesized 12 new analogues, two of which were active against both R Mtb and NR Mtb with MIC values of 12.5μg/mL, which would lead to further optimization for more potent anti-TB candidates.
- Mycobacterium tuberculosis,
- (+)-Calanolide A,
- N-Oxide heterocycle,
- Benzoimidazole,
- Bioreductive drug
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沈阳化工大学材料科学与工程学院沈阳 110142