Absztrakt Surface powder sticking in pharmaceutical mixing vessels poses a risk to the uniformity and quality of drug formulations. This study explores methods for evaluating the amount of pharmaceutical powder mixtures adhering to the metallic surfaces. Binary powder blends consisting…
Absztrakt β-Aminophosphonates obtained by the Michael addition of primary amines to the double bond of diethyl vinylphosphonate proved to be suitable starting materials (amine components) in the Kabachnik–Fields reaction with formaldehyde and dialkyl phosphites or secondary phosphine oxides to afford N-phosphonylmethyl-…
Absztrakt The synthesis of potentially biologically active phosphinoyl functionalized N-(2-(phenylethynyl)benzyl)amine, 1,2-dihydro-isoquinoline and 2H-isoindoline via a multicomponent reaction of 2-(phenylethynyl)benzaldehyde, amine and diphenylphosphine oxide is described for the first time. Depending on the catalyst and the conditions used, the same one-pot three-component reaction can…
Absztrakt Capsaicin and its derivatives are special alkaloids responsible for the pungency of spicy pepper fruits and are mainly used in the pharmaceutical, food, and cosmetic industries. Until now, only batch syntheses of capsaicin and some of its analogues have…
Absztrakt Exenatide (Ex4), a GLP-1 incretin mimetic polypeptide, is an effective therapeutic agent against diabetes and obesity. We highlight the indirect role of Ex4’s structure-stabilizing Trp-cage (Tc) motif in governing GLP-1 receptor (GLP-1R) signal transduction. We use various Ex4 derivatives…
Absztrakt Protein folds and the local environments they create can be compared using a variety of differently designed measures, such as the root mean squared deviation, the global distance test, the template modeling score or the local distance difference test.…
Absztrakt The most fundamental topological units of proteins are their autonomously folded domains. The rapid and reliable chemical synthesis of domains in the range of 5–10 kDa in size, remains a challenge. Their bacterial expression is cumbersome, especially when chemical…
Absztrakt Methods from artificial intelligence (AI), in general, and machine learning, in particular, have kept conquering new territories in numerous areas of science. Most of the applications of these techniques are restricted to the classification of large data sets, but…
Absztrakt Pseudoproline derivatives such as Thr(ΨPro)-OH are commonly used in peptide synthesis to reduce the likelihood of peptide aggregation and to prevent aspartimide (Asi) formation during the synthesis process. In this study, we investigate notable by-products such as aspartimide formation…
Absztrakt Aggregation-prone-motifs (APRs) of proteins are short segments, which – as isolated peptides – form diverse amyloid-like crystals. We introduce two APRs – designed variants of the incretin mimetic Exendin-4 – that both display crystal-phase polymorphism. Crystallographic and spectroscopic analysis…