Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 42, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2021.128088
Keywords
Adjuvant; Efflux pumps; Multidrug resistance; Mycobacterium tuberculosis
Categories
Funding
- Coordination for the Improvement of Higher Education Personnel (CAPES)
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NUNL02 has the potential to increase the susceptibility of multidrug resistant Mycobacterium tuberculosis strains to anti-TB drugs, possibly by affecting the efflux mechanism and killing the bacillus under nutrient deprivation. This compound shows promise as a new adjuvant for TB treatment.
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 2,2,2trifluoro-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.
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