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

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-β-carboline derivatives synthesized by the splice method are shown to have a...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2022-04, Vol.27 (9), p.2888
Main Authors: Liang, Yan, Song, Tianzeng, He, Bingmei, Tang, Lei, Zhou, Deshun, He, Dian
Format: Article
Language:English
Subjects:
Amino acids
Animals
Anti-Bacterial Agents - pharmacology
Antiinfectives and antibacterials
Bacteria
bacteriostatic experiment
Binding
Binding sites
Carbolines
Cattle
chemical synthesis
Crystal structure
Economic impact
Energy
Female
Flavin
Gram-negative bacteria
Gram-positive bacteria
Harmine - pharmacology
Humans
Hydrocarbons
Hydrogen bonding
Hydrogen bonds
Ligands
Mastitis
Mastitis, Bovine - drug therapy
Mastitis, Bovine - microbiology
Microorganisms
Minimum inhibitory concentration
Molecular docking
Molecular Docking Simulation
Proteins
Reagents
single crystal diffraction
Single crystals
Streptococcus
Streptococcus dysgalactiae
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Summary: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-β-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 ( , , and ) showed that compound had the best bacteriostatic effect on , with a mic value of 43.7 μ g/mL. When the concentration of was 1 × MIC and 2 × MIC, it had a significant inhibitory effect on , and there was almost no growth of at 4 × MIC. The binding properties of target compound to protein were simulated by the molecular docking technique. The ligand 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.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules27092888