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Synthesis and Antibacterial Study of Novel Harmine Derivatives and Tetrahydro-beta-Carboline Derivatives In Vitro

文献类型： 外文期刊

作者： Liang, Yan 1 ; Song, Tianzeng 2 ; He, Bingmei 2 ; Tang, Lei 1 ; Zhou, Deshun 3 ; He, Dian 1 ;

作者机构： 1.Lanzhou Univ, Sch Pharm, West Donggang Rd 199, Lanzhou 730000, Peoples R China

2.Tibet Acad Agr & Anim Husb Sci, Inst Anim Sci, Lhasa 850009, Peoples R China

3.Chinese Acad Agr Sci, Key Lab Vet Pharmaceut Dev, Minist Agr & Rural Affairs, Lanzhou Inst Husb & Pharmaceut Sci, 335 Qilihe Dist, Lanzhou 730050, Peoples R China

关键词： single crystal diffraction; chemical synthesis; bacteriostatic experiment; molecular docking

期刊名称：MOLECULES （ 影响因子：4.927； 五年影响因子：5.11 ）

ISSN：

年卷期： 2022 年 27 卷 9 期

页码：

收录情况： SCI

摘要： Dairy mastitis is a disease of dairy cattle caused by a variety of pathogenic microorganisms which has biought huge economic losses aused huge economic losses to the world. In this paper, Harmine derivatives and tetrahydro-beta-carboline derivatives synthesized by the splice method are shown to have a good inhibitory effect on the pathogenic bacteria of dairy mastitis. The results of a bacteriostatic test on pathogenic bacteria of dairy cow mastitis (S. dysgalactiae, S. pyogenes, B. subtilis and P. vulgaris) showed that compound 7l had the best bacteriostatic effect on Streptococcus dysgalactiae, with a mic value of 43.7 mu g/mL. When the concentration of 7l was 1 x MIC and 2 x MIC, it had a significant inhibitory effect on Streptococcus dysgalactiae, and there was almost no growth of Streptococcus dysgalactiae at 4 x MIC. The binding properties of target compound 7l to amine oxidase [flavin-containing] A protein were simulated by the molecular docking technique. The ligand 7l achieved strong binding with the receptor through three hydrogen bonds. The hydrogen bonds were amino acid residues thr-52, arg-51 and ser-24, which are the main force for the compound to bind to active sites.

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[1]Synthesis and Antibacterial Study of Novel Harmine Derivatives and Tetrahydro-beta-Carboline Derivatives In Vitro. Liang, Yan,Tang, Lei,He, Dian,Song, Tianzeng,He, Bingmei,Zhou, Deshun. 2022

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