Custodio Leite Talita O, Novais Juliana S, C de Carvalho Beatriz Lima, F Dias Flaviana Rodrigues, C Martins Nathalia R, da Silva Aldo Rodrigues, Geraldo Reinaldo Barros, da Conceição Nayra Cordeiro, Ratcliffe Norman, Ferreira Vitor F, Castro Helena C, Cunha Anna C
Universidade Federal Fluminense, Instituto de Química, Departamento de Química Orgânica, Programa de Pós-Graduação em Química, 24020-141, Niterói, Rio de Janeiro, Brasil.
Universidade Federal Fluminense, Programa de Pós-graduação em Patologia, Hospital Universitário Antônio Pedro, 24033-900, Niterói, Rio de Janeiro, Brasil.
Future Med Chem. 2024;16(21):2247-2261. doi: 10.1080/17568919.2024.2400954. Epub 2024 Oct 14.
This work describes the synthesis and antimicrobial evaluation of 6-aminated 1,4-benzoquinones (6-AQs) against seven resistant pathogens. The 6-AQs, synthesized via a Michael addition reaction between bromoquinone and -substituted anilines, were assessed for their antimicrobial activity through both and analyses. Bromoquinone and 6-AQs with electron-withdrawing groups demonstrated activity against , with minimum inhibitory concentrations ranging from 16 to 128 μg/ml, comparable to standard antimicrobials. Two derivatives exhibited minimum inhibitory concentrations values against methicillin-resistant ranging from 64 to 128 μg/ml. These compounds demonstrated both bacteriostatic and bactericidal effects, and antibiofilm features. The 6-AQs and showed a promising antimicrobial profile, indicating their potential as new therapeutic options.
这项工作描述了6-氨基-1,4-苯醌(6-AQs)对七种耐药病原体的合成及抗菌评估。通过溴醌与取代苯胺之间的迈克尔加成反应合成的6-AQs,通过肉汤稀释法和纸片扩散法分析评估了它们的抗菌活性。具有吸电子基团的溴醌和6-AQs对金黄色葡萄球菌表现出活性,最低抑菌浓度范围为16至128μg/ml,与标准抗菌剂相当。两种衍生物对耐甲氧西林金黄色葡萄球菌的最低抑菌浓度值范围为64至128μg/ml。这些化合物表现出抑菌和杀菌作用以及抗生物膜特性。6-AQs和表现出有前景的抗菌谱,表明它们作为新治疗选择的潜力。