Introduction: In hypo-albuminemia, the extent of albumin binding of a drug decreases. The resulting change in plasma protein binding only rarely leads to clinically relevant changes in unbound drug exposure. Nevertheless, in the critically ill, a tendency to increase dosing of anti-infective therapy is seen in patients experiencing hypo-albuminemia...
Published in Gut
CRD42015025445.
The development of straightforward and versatile peptide cyclisation methods is highly desired to meet the demand for more stable peptide-based drugs. Herein, a new method for the synthesis of side-chain-to-tail cyclic peptides with the simultaneous introduction of an N-terminal handle, based on the introduction of an N-terminal thiolactone buildin...
Reduced antimicrobial susceptibility due to resistance and tolerance has become a serious threat to human health. An approach to overcome this reduced susceptibility is the use of antibiotic adjuvants, also known as potentiators. These are compounds that have little or no antibacterial effect on their own but increase the susceptibility of bacteria...
The anodic voltammetric behavior of an antibiotic drug, lincomycin hydrochloride (LIN) at gold electrode (GE) has been investigated using cyclic and linear sweep voltammetry. The dependence of the current on pH, concentration and scan rate were investigated to optimize the experimental conditions for the determination of lincomycin. The anodic peak...
The HauserKraus reaction of sulfonyl phthalide with nitroalkene derivatives provides access to aminophenanthrenes, including phenanthrene-substituted amino acids and benzoquinolines. The intermediate quinones bearing a key ketoalkyl moiety undergoes facile intramolecular enamine cyclization. Interestingly, enamines derived from primary and secondar...
Microcin C7 (McC), widely distributed in enterobacteria, is a promising antibiotic against antibiotic resistance. Previous studies have demonstrated that the heptapeptide of McC is only responsible for recognizing the inner membrane transporter YejABEF to deliver McC into microbial cells, but lacks the capacity for inhibiting microbial cell growth....
Teixobactin is a highly promising antibacterial depsipeptide consisting of four D-amino acids and a rare L-allo-enduracididine amino acid. L-allo-Enduracididine is reported to be important for the highly potent antibacterial activity of teixobactin. However, it is also a key limiting factor in the development of potent teixobactin analogues due to ...
Several B. cenocepacia mouse models are available to study the pulmonary infection by this Burkholderia cepacia complex (BCC) species. However, a characterized B. cenocepacia mouse model to evaluate the efficacy of potential new antibacterial therapies is not yet described. Therefore, we optimized and validated the course of infection (Le. bacteria...
