Synthesis and Structure-Activity Relationships ofNovel Amino/Nitro Substituted 3-Arylcoumarins asAntibacterial Agents

Molecules

Maria J. Matos¹  Saleta Vazquez-Rodriguez¹  Lourdes Santana¹  Eugenio Uriarte¹  Cristina Fuentes-Edfuf¹  Ysabel Santos¹ 

[1] ¹Departamento de Química Orgánica, Facultad de Farmacia, Universidad de Santiago de Compostela, 15782 Santiago de Compostela, Spain ²Departamento de Microbiología y Parasitología, Facultad de Biología, Universidad de Santiago de Compostela, 15782 Santiago de Compostela, Spain

关键词: amino/nitro substituted 3-arylcoumarins;    Perkin reaction;    antibacterial assays;    S. aureus;    E. coli;   

DOI  :  10.3390/molecules18021394

来源: mdpi

【 摘 要 】

A new series of amino/nitro-substituted 3-arylcoumarins were synthesized and their antibacterial activity against clinical isolates of Staphylococcus aureus (Gram-positive) and Escherichia coli (Gram-negative) was evaluated. Some of these molecules exhibited antibacterial activity against S. aureus comparable to the standards used (oxolinic acid and ampicillin). The preliminary structure-activity relationship (SAR) study showed that the antibacterial activity against S. aureus depends on the position of the 3-arylcoumarin substitution pattern. With the aim of finding the structural features for the antibacterial activity and selectivity, in the present manuscript different positions of nitro, methyl, methoxy, amino and bromo substituents on the 3-arylcoumarin scaffold were reported.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.