首页|Amino ether analogues of 4,4′-dihydroxy-3-methoxy-6,7′-cyclolignan and their activity against drug-resistant bacteria
Amino ether analogues of 4,4′-dihydroxy-3-methoxy-6,7′-cyclolignan and their activity against drug-resistant bacteria
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NSTL
Elsevier
? 2022 Phytochemical Society of EuropeLarrea tridentata antibacterial lignan 4,4′-dihydroxy-3-methoxy-6,7′-cyclolignan (1) was derivatized to obtain eleven new amino ether derivatives (2 A-12 C). The structural elucidation of compounds was performed by analysis of 1D- and 2D NMR spectral data and HRESIMS. The antibacterial activity of compounds was determined against nine drug-resistant bacteria and two strains of Mycobacterium tuberculosis (sensitive ATCC 27294 H37Rv and drug-resistant G122). Results showed that all derivatives were devoid of activity towards six gram-negative clinical isolates assayed. However, seven derivatives displayed antibacterial activity against three gram-positive drug-resistant bacteria. Further, enhancement of antibacterial activity was only observed for the compounds 2 A and 10 C-12 C (MIC of 12.5 μg/mL) which were two-fold more active than the starting material 1 against vancomycin-resistant Enterococcus faecium. All derivatives, except compound 9 B, showed antitubercular activity against both M. tuberculosis strains. Interestingly, all the compounds, except for 2 A and 11 A, were more active than the starting material 1 (MIC of 50 μg/mL). Compound 4 C was the only compound as active as the positive control ethambutol against the drug-resistant strain M. tuberculosis G122 (MIC of 6.25 μg/mL). In addition, the derivative 7 C was the most active compound against the sensitive strain M. tuberculosis H37Rv (MIC of 6.25 μg/mL)
Nunez-Mojica G.、Hernandez-Carrillo M.L.、Avalos-Alanis F.G.、Camacho-Corona M.D.R.、Garza-Gonzalez E.、Rivas-Galindo V.M.、Silva-Mares D.A.、Bazin M.-A.、Marchand P.
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Facultad de Ciencias Químicas Universidad Autonoma de Nuevo Leon
Departamento de Bioquímica y Medicina Molecular Facultad de Medicina/Hospital Universitario Dr. José Eleuterio González Universidad Autonoma de Nuevo Leon Madero y Aguirre Peque?o Mitras Centro
Departamento de Química Analítica Facultad de Medicina Universidad Autonoma de Nuevo Leon. Madero y Aguirre Peque?o Mitras Centro
Nantes Université Cibles et médicaments des infections et de l′immunité IICiMed
NSTL
Elsevier
