Pereira, Ulisses A.’s team published research in European Journal of Medicinal Chemistry in 2014-07-23 | CAS: 127972-00-3

European Journal of Medicinal Chemistry published new progress about Antibacterial agents. 127972-00-3 belongs to class ethers-buliding-blocks, name is 2-Methoxy-5-methylphenylboronic acid, and the molecular formula is C8H11BO3, Recommanded Product: 2-Methoxy-5-methylphenylboronic acid.

Pereira, Ulisses A. published the artcileInhibition of Enterococcus faecalis biofilm formation by highly active lactones and lactams analogs of rubrolides, Recommanded Product: 2-Methoxy-5-methylphenylboronic acid, the main research area is Enterococcus biofilm inhibition rubrolide analog; Anti-biofilm activity; Quorum sensing antagonist; Rubrolides; γ-Alkylidene-γ-lactams; γ-Alkylidene-γ-lactones; γ-Hydroxy-γ-lactams.

Seven β-aryl substituted γ-alkylidene-γ-lactones analogs of rubrolides were synthesized from mucobromic acid and converted through a lactamization with isobutylamine into their corresponding γ-hydroxy-γ-lactams (76-85%). These lactams were converted into (Z)- and (E)-γ-alkylidene-γ-lactams (23-45%). All compounds were fully characterized by IR, NMR (1H and 13C), COSY and HETCOR bidimensional experiments, and NOE difference spectroscopy experiments when necessary. Evaluation of these three different classes of compounds against Enterococcus faecalis biofilm formation showed that all classes are active and the highest biofilm inhibition activity was caused by lactam 13f (IC50 = 0.76 μg/mL). Moreover, in almost all cases at least one of the lactams is more active than its correspondent γ-alkylidene-γ-lactone. The use of rubrolides as a lead structure has proven successful for the identification of new compounds displaying novel antibacterial activities, namely biofilm inhibition, which have the potential for the development of antimicrobial drugs targeted to inhibition of the initial stages of bacterial infections, rather than bacterial viability. Such drugs are less prompt to induce bacterial resistance, being therefore a more cost-effective investment for pharmaceutical research.

European Journal of Medicinal Chemistry published new progress about Antibacterial agents. 127972-00-3 belongs to class ethers-buliding-blocks, name is 2-Methoxy-5-methylphenylboronic acid, and the molecular formula is C8H11BO3, Recommanded Product: 2-Methoxy-5-methylphenylboronic acid.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem