61 documents found, page 1 of 7
Development of polymyxin B derivatives incorporating uncommon amino acids: synt...
Linhares, Mariana Esteves; Costa, Susana Paula; Lopes, Susana PatríciaThe alarming rise of antimicrobial resistance (AMR) and multidrug-resistant (MDR) Gram-negative bacteria led the World Health Organization (WHO) to publish a list of pathogens for which the development of new antibiotics is urgent. Some bacteria have been prioritized as they are resistant to more than three classes of antibiotics, such as the ESKAPE group that includes Gram-positive bacteria (Enterococcus faeci...
Polymyxin B as scaffold for new analogues bearing uncommon amino acids: synthes...
Linhares, Mariana; Lopes, Susana Patrícia; Costa, Susana P.The alarming rise of antimicrobial resistance (AMR) and multidrug-resistant (MDR) Gram-negative bacteria led the World Health Organization (WHO) to publish a list of pathogens for which the development of new antibiotics is urgent. Some bacteria have been prioritized as they are resistant to more than three classes of antibiotics, such as the ESKAPE group that includes Gram-positive bacteria (Enterococcus faeci...
Co-immobilization of ciprofloxacin and chlorhexidine as a broad-spectrum antimi...
Alves, Diana Filipa Barros; Pereira, Maria Olívia; Lopes, Susana PatríciaThe endotracheal tube (ETT) affords support for intubated patients, but the increasing incidence of ventilator-associated pneumonia (VAP) is jeopardizing its application. ETT surfaces promote (poly)microbial colonization and biofilm formation, with a heavy burden for VAP. Devising safe, broad-spectrum antimicrobial materials to tackle the ETT bioburden is needful. Herein, we immobilized ciprofloxacin (CIP) and/...
Synthesis of polymyxin analogs with enhanced activity towards Gram-negative bio...
Grainha, Tânia; Martins, Elsa; Costa, Susana Paula; Jorge, Paula; Lopes, Susana Patrícia[Excerpt] Polymyxins (PM) B and E are last-resort drugs against Gram-negative bacterial infections (often biofilm-related), but resistance and toxicity compromise PM use. A fast-growing no. of PM analogs have been reported, but with varied success in improving PM activity and ameliorating toxicity. ,-Dialkylglycines (DAG), unnatural amino acids, hold unique characteristics (bioactivity, metabolic resistance, hy...
Ddevelopment of next-generation polymyxins targeting problematic gram-negative ...
Graínha, Tânia Raquel Rodrigues; Martins, Elsa; Costa, Susana P.; Jorge, Paula; Lopes, Susana PatríciaAntimicrobial resistance is a major global health threat, with which the antibiotic discovery pipeline is not keeping up. Polymyxins (PM) B and E have resurrected as last-resort drugs (given their toxicity) against Gram-negative bacterial infections, but PM resistance has already been reported, resulting in the lack of effective therapies. Taking advantage of these valuable scaffolds, we set out to design new P...
Novel polymyxin analogs with promising activity against Gram-negative bacterial...
Graínha, Tânia Raquel Rodrigues; Martins, Elsa; Costa, Susana P.; Jorge, Paula; Lopes, Susana PatríciaAntimicrobial resistance is a major global health threat, with which the antibiotic discovery pipeline is not keeping up. Polymyxins (PM) B and E have resurrected as last-resort drugs (given their toxicity) against Gram-negative bacterial infections, but PM resistance has already been reported [1], resulting in the lack of effective therapies. Taking advantage of these valuable scaffolds, we set out to design n...
Incorporation of unnatural alpha,alpha-dialkylglycines in polymyxins: synthesis...
Martins, Elsa; Jorge, Paula; Lopes, Susana Patrícia; Costa, Susana P.Lower respiratory infections caused by Gram-negative pathogens classified by the WHO as priority targets (e.g. Pseudomonas aeruginosa, Acinetobacter baumannii, Klebsiella pneumoniae) pose a great concern as they are often mediated by recalcitrant polymicrobial biofilms and multidrug resistant (MDR) strains. Current antibiotics, and antibacterial agents in clinical development, remain ineffective against these b...
Antimicrobial materials for endotracheal tubes: a review on the last two decade...
Alves, Diana Filipa Barros; Graínha, Tânia Raquel Rodrigues; Pereira, Maria Olívia; Lopes, Susana PatríciaVentilator-associated pneumonia (VAP) is an unresolved problem in nosocomial settings, remaining consistently associated with a lack of treatment, high mortality, and prolonged hospital stay in mechanically ventilated patients. The endotracheal tube (ETT) is the major culprit for VAP development owing to its early surface microbial colonization and biofilm formation by multiple pathogens, both critical events f...
A cyclic dab analogue by an ugi multicomponent reaction
Martins, Elsa M. T.; Jorge, Paula; Lopes, Susana Patrícia; Costa, Susana P.Peptides regulate virtually all physiological processes and the design of peptides with pharmacological interest is a current thrust of the pharma industry. It is therefore desirable that the peptides have enzymatic stability to increase their bioavailability and enhance their efficacy. One strategy is to modify the native sequence of biologically active peptides by introducing unnatural amino acids, to obtain ...
Discerning the role of polymicrobial biofilms in the ascent, prevalence, and ex...
Lopes, Susana Patrícia; Jorge, Paula Alexandra Silva; Sousa, Ana Margarida; Pereira, Maria OlíviaAntimicrobial therapy is facing a worrisome and underappreciated challenge, the phenomenon of heteroresistance (HR). HR has been gradually documented in clinically relevant pathogens (e.g. Pseudomonas aeruginosa, Staphylococcus aureus, Burkholderia spp., Acinetobacter baumannii, Klebsiella pneumoniae, Candida spp.) towards several drugs and is believed to complicate the clinical picture of chronic infections. T...