da Silva Maria M C, de Araújo-Neto José B, de Araújo Ana C J, Freitas Priscilla R, de M Oliveira-Tintino Cícera D, Begnini Iêda M, Rebelo Ricardo A, da Silva Luiz E, Mireski Sandro L, Nasato Michele C, Krautler Maria I L, Ribeiro-Filho Jaime, Coutinho Henrique D M, Tintino Saulo R
Laboratory of Microbiology and Molecular Biology (LMBM), Department of Biological Chemistry, Regional University of Cariri-URCA, Rua Cel. Antonio Luiz, 1161. Pimenta, Crato, CE CEP: 63105-000 Brazil.
Department of Chemistry, Regional University of Blumenau-FURB, Blumenau, Brazil.
Indian J Microbiol. 2021 Mar;61(1):100-103. doi: 10.1007/s12088-020-00910-6. Epub 2020 Oct 10.
This study aimed to evaluate the intrinsic antibacterial activity and antibiotic-enhancing effect of an arylamino methylene derivative (MAD) in association with fluoroquinolones. The antibacterial activity against multiresistant , and was analyzed by determining the minimum inhibitory concentration (MIC) using the broth micro dilution method. A reduction in the MIC of the fluoroquinolones against strains treated simultaneously with the MAD was interpreted as an enhanced antibiotic activity. While the MAD exhibited no clinically effective action (MIC ≥ 1.024 µg/mL), it was found to significantly potentiate the activity of norfloxacin, ofloxacin and lomefloxacin against all the strains, which may be related to structural similarities between the MAD and quinolones. Our findings suggest that Meldrum's acid arylamino derivatives may represent promising molecules in the elaboration of new drugs to reverse resistance to fluoroquinolones.
本研究旨在评估一种芳基氨基亚甲基衍生物（MAD）与氟喹诺酮类药物联合使用时的内在抗菌活性及抗生素增强作用。采用肉汤微量稀释法测定最低抑菌浓度（MIC），分析其对多重耐药菌、 及 的抗菌活性。氟喹诺酮类药物对同时用MAD处理的菌株的MIC降低被解释为抗生素活性增强。虽然MAD未表现出临床有效作用（MIC≥1.024μg/mL），但发现它能显著增强诺氟沙星、氧氟沙星和洛美沙星对所有菌株的活性，这可能与MAD和喹诺酮类药物之间的结构相似性有关。我们的研究结果表明，丙二酸亚异丙酯芳基氨基衍生物可能是开发逆转对氟喹诺酮类药物耐药性的新药的有前景的分子。
