Cargando…
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...
Autores principales: | , , , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9104299/ https://www.ncbi.nlm.nih.gov/pubmed/35566239 http://dx.doi.org/10.3390/molecules27092888 |
_version_ | 1784707760554770432 |
---|---|
author | Liang, Yan Song, Tianzeng He, Bingmei Tang, Lei Zhou, Deshun He, Dian |
author_facet | Liang, Yan Song, Tianzeng He, Bingmei Tang, Lei Zhou, Deshun He, Dian |
author_sort | Liang, Yan |
collection | PubMed |
description | 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 (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 μ g/mL. When the concentration of 7l was 1 × MIC and 2 × MIC, it had a significant inhibitory effect on Streptococcus dysgalactiae, and there was almost no growth of Streptococcus dysgalactiae at 4 × 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. |
format | Online Article Text |
id | pubmed-9104299 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-91042992022-05-14 Synthesis and Antibacterial Study of Novel Harmine Derivatives and Tetrahydro-β-Carboline Derivatives In Vitro Liang, Yan Song, Tianzeng He, Bingmei Tang, Lei Zhou, Deshun He, Dian Molecules Article 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 (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 μ g/mL. When the concentration of 7l was 1 × MIC and 2 × MIC, it had a significant inhibitory effect on Streptococcus dysgalactiae, and there was almost no growth of Streptococcus dysgalactiae at 4 × 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. MDPI 2022-04-30 /pmc/articles/PMC9104299/ /pubmed/35566239 http://dx.doi.org/10.3390/molecules27092888 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Liang, Yan Song, Tianzeng He, Bingmei Tang, Lei Zhou, Deshun He, Dian Synthesis and Antibacterial Study of Novel Harmine Derivatives and Tetrahydro-β-Carboline Derivatives In Vitro |
title | Synthesis and Antibacterial Study of Novel Harmine Derivatives and Tetrahydro-β-Carboline Derivatives In Vitro |
title_full | Synthesis and Antibacterial Study of Novel Harmine Derivatives and Tetrahydro-β-Carboline Derivatives In Vitro |
title_fullStr | Synthesis and Antibacterial Study of Novel Harmine Derivatives and Tetrahydro-β-Carboline Derivatives In Vitro |
title_full_unstemmed | Synthesis and Antibacterial Study of Novel Harmine Derivatives and Tetrahydro-β-Carboline Derivatives In Vitro |
title_short | Synthesis and Antibacterial Study of Novel Harmine Derivatives and Tetrahydro-β-Carboline Derivatives In Vitro |
title_sort | synthesis and antibacterial study of novel harmine derivatives and tetrahydro-β-carboline derivatives in vitro |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9104299/ https://www.ncbi.nlm.nih.gov/pubmed/35566239 http://dx.doi.org/10.3390/molecules27092888 |
work_keys_str_mv | AT liangyan synthesisandantibacterialstudyofnovelharminederivativesandtetrahydrobcarbolinederivativesinvitro AT songtianzeng synthesisandantibacterialstudyofnovelharminederivativesandtetrahydrobcarbolinederivativesinvitro AT hebingmei synthesisandantibacterialstudyofnovelharminederivativesandtetrahydrobcarbolinederivativesinvitro AT tanglei synthesisandantibacterialstudyofnovelharminederivativesandtetrahydrobcarbolinederivativesinvitro AT zhoudeshun synthesisandantibacterialstudyofnovelharminederivativesandtetrahydrobcarbolinederivativesinvitro AT hedian synthesisandantibacterialstudyofnovelharminederivativesandtetrahydrobcarbolinederivativesinvitro |