2,2,2-trifluoro-1-(1,4,5,6-tetrahydropyridin-3-yl)ethanone derivative as efflux pump inhibitor in Mycobacterium tuberculosis
[Display omitted] 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 putati...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2021-06, Vol.42, p.128088-128088, Article 128088 |
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| creator | Halicki, Priscila Cristina Bartolomeu Vianna, Júlia Silveira Zanatta, Nilo de Andrade, Valquiria Pereira de Oliveira, Mariana Mateus, Malu da Silva, Marcos Vinicius Rodrigues, Virmondes Ramos, Daniela Fernandes Almeida da Silva, Pedro Eduardo |
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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. |
| doi_str_mv | 10.1016/j.bmcl.2021.128088 |
| format | Article |
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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.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2021.128088</identifier><identifier>PMID: 33964440</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Adjuvant ; Efflux pumps ; Multidrug resistance ; Mycobacterium tuberculosis</subject><ispartof>Bioorganic & medicinal chemistry letters, 2021-06, Vol.42, p.128088-128088, Article 128088</ispartof><rights>2021 Elsevier Ltd</rights><rights>Copyright © 2021 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c356t-fa2c73ceed743e94b59ac07efcc89a9e94055d53262a13ce9e5e2859b481fd233</citedby><cites>FETCH-LOGICAL-c356t-fa2c73ceed743e94b59ac07efcc89a9e94055d53262a13ce9e5e2859b481fd233</cites><orcidid>0000-0002-6849-1702</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2021.128088$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/33964440$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Halicki, Priscila Cristina Bartolomeu</creatorcontrib><creatorcontrib>Vianna, Júlia Silveira</creatorcontrib><creatorcontrib>Zanatta, Nilo</creatorcontrib><creatorcontrib>de Andrade, Valquiria Pereira</creatorcontrib><creatorcontrib>de Oliveira, Mariana</creatorcontrib><creatorcontrib>Mateus, Malu</creatorcontrib><creatorcontrib>da Silva, Marcos Vinicius</creatorcontrib><creatorcontrib>Rodrigues, Virmondes</creatorcontrib><creatorcontrib>Ramos, Daniela Fernandes</creatorcontrib><creatorcontrib>Almeida da Silva, Pedro Eduardo</creatorcontrib><title>2,2,2-trifluoro-1-(1,4,5,6-tetrahydropyridin-3-yl)ethanone derivative as efflux pump inhibitor in Mycobacterium tuberculosis</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>[Display omitted]
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. 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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.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>33964440</pmid><doi>10.1016/j.bmcl.2021.128088</doi><tpages>1</tpages><orcidid>https://orcid.org/0000-0002-6849-1702</orcidid></addata></record> |
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| source | ScienceDirect Journals (5 years ago - present) |
| subjects | Adjuvant Efflux pumps Multidrug resistance Mycobacterium tuberculosis |
| title | 2,2,2-trifluoro-1-(1,4,5,6-tetrahydropyridin-3-yl)ethanone derivative as efflux pump inhibitor in Mycobacterium tuberculosis |
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