[:pb]Authors: Moraes, A. M.; Da Silva, E. T. ; Wardell, J. L. ; De Souza, M. V. N.
Source: Chemistry of Natural Compounds, v. 56, p. 633-638, 2020
Publisher: Springer
Abstract
In this work, we report the first-time assessment of o-eugenol, 6-allyl-2-methoxyphenol, and their selected derivatives, against Mycobacterium tuberculosis H37RV, using the MABA susceptibility test. The bromo, nitro, O-alkylated, and reduced derivatives were obtained by standard methods and were characterized by spectroscopic and mass spectral data. Structure–activity relationships were investigated, with the most active derivatives being 4,5-dibromo-2-methoxy-6-propylphenol (139 μM) and 2-methoxy-3-nitro-6-propylphenol (237 μM). This study provides important information on the rational design of new lead anti-TB drugs based on o-eugenol derivatives.
Keywords: eugenol, o-eugenol, synthesis, tuberculosis, Mycobacterium tuberculosis, nitration, bromination, large scale
Document Type: Research Article
DOI: 10.1007/s10600-020-03110-2
Publication date: 24 de julho de 2020[:]
