期刊
MOLECULES
卷 22, 期 9, 页码 -出版社
MDPI
DOI: 10.3390/molecules22091457
关键词
Mycobacterium tuberculosis; mechanochemistry; hydrazone
资金
- CNRS
- University Paul Sabatier
- grant VEGA [1/0284/15]
A series of isoniazid derivatives bearing a phenolic or heteroaromatic coupled frame were obtained by mechanochemical means. Their pH stability and their structural (conformer/isomer) analysis were checked. The activity of prepared derivatives against Mycobacterium tuberculosis cell growth was evaluated. Some compounds such as phenolic hydrazine 1a and almost all heteroaromatic ones, especially 2, 5 and 7, are more active than isoniazid, and their activity against some M. tuberculosis MDR clinical isolates was determined. Compounds 1a and 7 present a selectivity index > 1400 evaluated on MRC5 human fibroblast cells. The mechanism of action of selected hydrazones was demonstrated to block mycolic acid synthesis due to InhA inhibition inside the mycobacterial cell.
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