- Synthesis of covalent bonding MWCNT-oligoethylene linezolid conjugates and their antibacterial activity against bacterial strains
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Nowadays, infectious diseases caused by drug-resistant bacteria have become especially important. Linezolid is an antibacterial drug active against clinically important Gram positive strains; however, resistance showed by these bacteria has been reported. Nanotechnology has improved a broad area of science, such as medicine, developing new drug delivery and transport systems. In this work, several covalently bounded conjugated nanomaterials were synthesized from multiwalled carbon nanotubes (MWCNTs), a different length oligoethylene chain (Sn), and two linezolid precursors (4and7), and they were evaluated in antibacterial assays. Interestingly, due to the intrinsic antibacterial activity of the amino-oligoethylene linezolid analogues, these conjugated nanomaterials showed significant antibacterial activity against various tested bacterial strains in a radial diffusion assay and microdilution method, including Gram negative strains asEscherichia coli(11 mm, 6.25 μg mL?1) andSalmonella typhi(14 mm, ≤0.78 μg mL?1), which are not inhibited by linezolid. The results show a significant effect of the oligoethylene chain length over the antibacterial activity. Molecular docking of amino-oligoethylene linezolid analogs shows a more favorable interaction of theS2-7analog in the PTC ofE. coli.
- Alatorre-Barajas, José A.,Alcántar-Zavala, Eleazar,Alonso-Nú?ez, Gabriel,Cabrera, Alberto,Estrada-Zavala, Edgar,Gil-Rivas, M. Graciela,Gochi-Ponce, Y.,Medina-Franco, J. L.,Montes-ávila, Julio,Ochoa-Terán, Adrián,Reynoso-Soto, Edgar A.,Rivera-Lugo, Yazmin Yorely,Trujillo-Navarrete, Balter
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p. 28912 - 28924
(2021/09/22)
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- Preparation methods of medicine linezolid for treating bacteremia and crystal form VI of medicine linezolid
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The invention discloses preparation methods of a medicine linezolid for treating bacteremia and a crystal form VI of the medicine linezolid. The crystal form VI of the medicine linezolid for treatingthe bacteremia is prepared from the medicine linezolid for treating the bacteremia. The preparation method comprises the following steps of putting the medicine linezolid for treating the bacteremia into a ball milling jar according to that every 100mg of the medicine linezolid for treating the bacteremia is added into 10mu L to 20mu L of tetrahydrofuran, and milling for 40min to 90min with the milling frequency of 6HZ to 12HZ, so as to obtain the crystal form VI of the medicine linezolid for treating the bacteremia. The preparation method adopts a preparation technique in which raw materialsare easily obtained, which is economical and environmentally friendly and the quality is further superior; the reaction yield is improved; further, the optical purity of the crystal form VI of the medicine linezolid for treating the bacteremia, which is prepared and obtained by the method, through the cooperation of the milling frequency and a milling time is 99.5 percent or above, and the qualityof a product is greatly improved.
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Paragraph 0026; 0027; 0028
(2019/04/11)
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