Synthesis and structure-activity relationships of  novel amino/nitro substituted 3-arylcoumarins as  antibacterial agents.
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.
Departamento de Química Orgánica, Facultad de Farmacia, Universidad de Santiago de Compostela, 15782 Santiago de Compostela, Spain. mariacmatos@gmail.com
Maria J
MJ
Matos
Saleta
S
Vazquez-Rodriguez
Lourdes
L
Santana
Eugenio
E
Uriarte
Cristina
C
Fuentes-Edfuf
Ysabel
Y
Santos
Angeles
A
Muñoz-Crego
D000588:Amines / Q000737:chemistry*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001728:Dicumarol / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004926:Escherichia coli / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D009574:Nitro Compounds / Q000737:chemistry*; D009675:Novobiocin / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship
D000588:Amines; D000900:Anti-Bacterial Agents; D003374:Coumarins; D009574:Nitro Compounds; D009675:Novobiocin; D001728:Dicumarol