2,2,2-trifluoro-1-(1,4,5,6-tetrahydropyridin-3-yl)ethanone derivative as efflux pump inhibitor in Mycobacterium tuberculosis
Priscila Cristina Bartolomeu Halicki
1
,
Júlia Silveira Vianna
1
,
Nilo Zanatta
2
,
Valquiria Pereira De Andrade
2
,
Mariana M. de Oliveira
3
,
Malu Mateus Santos Obata
3
,
Marcos Marques da Silva
3
,
Virmondes Rodrigues
3
,
Daniela Ramos
1
,
Pedro Eduardo Almeida da Silva
1
3
Departamento de Microbiologia, Imunologia e Parasitologia - Universidade Federal do Triângulo Mineiro (UFTM) - Avenida Frei Paulino, 30 - Nossa Senhora da Abadia. Uberaba, Minas Gerais CEP 38025-180, Brazil
|
Publication type: Journal Article
Publication date: 2021-06-01
scimago Q2
wos Q2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
33964440
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
Although the administration of combined therapy is efficient to tuberculosis (TB) treatment caused by susceptible Mycobacterium tuberculosis strains, to overcome the multidrug resistance is still a challenge. Some studies have reported evidence about tetrahydropyridines as a putative efflux pump inhibitor, including in mycobacteria, being a promising strategy against M. tuberculosis. Thus, we investigated the biological potential of 2,2,2-trifluoro-1-(1,4,5,6-tetrahydropyridin-3-yl)ethanone derivative (NUNL02) against two strains of M. tuberculosis. NUNL02 was able to increase the susceptibility of the multidrug resistant strain to the anti-TB drugs, resulting in synergism with rifampicin. Still, we assume that this compound plays a role in the efflux mechanism in M. tuberculosis, besides, to be able to kill the bacillus under the deprivation of essential nutrients. Thus, our findings highlight NUNL02 as a promising prototype to develop a new adjuvant for TB treatment, mainly as EPI.
Found
Nothing found, try to update filter.
Found
Nothing found, try to update filter.
Top-30
Journals
|
1
|
|
|
Tuberculosis
1 publication, 20%
|
|
|
Journal of Fluorine Chemistry
1 publication, 20%
|
|
|
European Journal of Organic Chemistry
1 publication, 20%
|
|
|
Tetrahedron Letters
1 publication, 20%
|
|
|
Pharmaceuticals
1 publication, 20%
|
|
|
1
|
Publishers
|
1
2
3
|
|
|
Elsevier
3 publications, 60%
|
|
|
Wiley
1 publication, 20%
|
|
|
MDPI
1 publication, 20%
|
|
|
1
2
3
|
- We do not take into account publications without a DOI.
- Statistics recalculated weekly.
Are you a researcher?
Create a profile to get free access to personal recommendations for colleagues and new articles.
Metrics
5
Total citations:
5
Citations from 2025:
1
(20%)
Cite this
GOST |
RIS |
BibTex
Cite this
GOST
Copy
Halicki P. C. B. et al. 2,2,2-trifluoro-1-(1,4,5,6-tetrahydropyridin-3-yl)ethanone derivative as efflux pump inhibitor in Mycobacterium tuberculosis // Bioorganic and Medicinal Chemistry Letters. 2021. Vol. 42. p. 128088.
GOST all authors (up to 50)
Copy
Halicki P. C. B., Vianna J. S., Zanatta N., De Andrade V. P., de Oliveira M. M., Mateus Santos Obata M., da Silva M. M., Rodrigues V., Ramos D., Almeida da Silva P. E. 2,2,2-trifluoro-1-(1,4,5,6-tetrahydropyridin-3-yl)ethanone derivative as efflux pump inhibitor in Mycobacterium tuberculosis // Bioorganic and Medicinal Chemistry Letters. 2021. Vol. 42. p. 128088.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1016/j.bmcl.2021.128088
UR - https://doi.org/10.1016/j.bmcl.2021.128088
TI - 2,2,2-trifluoro-1-(1,4,5,6-tetrahydropyridin-3-yl)ethanone derivative as efflux pump inhibitor in Mycobacterium tuberculosis
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Halicki, Priscila Cristina Bartolomeu
AU - Vianna, Júlia Silveira
AU - Zanatta, Nilo
AU - De Andrade, Valquiria Pereira
AU - de Oliveira, Mariana M.
AU - Mateus Santos Obata, Malu
AU - da Silva, Marcos Marques
AU - Rodrigues, Virmondes
AU - Ramos, Daniela
AU - Almeida da Silva, Pedro Eduardo
PY - 2021
DA - 2021/06/01
PB - Elsevier
SP - 128088
VL - 42
PMID - 33964440
SN - 0960-894X
SN - 1464-3405
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2021_Halicki,
author = {Priscila Cristina Bartolomeu Halicki and Júlia Silveira Vianna and Nilo Zanatta and Valquiria Pereira De Andrade and Mariana M. de Oliveira and Malu Mateus Santos Obata and Marcos Marques da Silva and Virmondes Rodrigues and Daniela Ramos and Pedro Eduardo Almeida da Silva},
title = {2,2,2-trifluoro-1-(1,4,5,6-tetrahydropyridin-3-yl)ethanone derivative as efflux pump inhibitor in Mycobacterium tuberculosis},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2021},
volume = {42},
publisher = {Elsevier},
month = {jun},
url = {https://doi.org/10.1016/j.bmcl.2021.128088},
pages = {128088},
doi = {10.1016/j.bmcl.2021.128088}
}