Abstract Applications of polar aprotic solvents are inevitable in the chemical industry, but few nonhazardous alternatives are available. Herein, we propose methyl sesamol (MeSesamol) as a promising new bio-based alternative for polar aprotic solvents and demonstrate its versatile applications. MeSesamol…
Abstract The recovery and reuse of the enantioselective catalysts produced by tedious work are important not only from the perspective of green chemistry, but also from the point of view of productivity. Some of the carbohydrate-based crown ethers prepared in…
Absztrakt A propylphosphonic anhydride (T3P®)-mediated new multicomponent method was developed for the synthesis of benzo[de]isoquinolinones bearing a phosphonate or a phosphine oxide moiety as a new family of compounds. The one-pot three-component reaction of 1,8-naphthalaldehydic acid, primary amines and dialkyl…
Abstract A focused library of 1-adamantyl arylthiophosphonates was prepared in racemic form. An enantioseparation method was developed for P-stereogenic thiophosphonates using (S)-1-phenylethylamine as the resolving agent. Under optimized conditions, three out of the five arylthiophosphonates were prepared in enantiopure form (ee >…
Absztrakt A series of new dialkyl α-diethylphosphonoylethyl-α-hydroxy-ethylphosphonates were prepared using the Pudovik reaction of the corresponding γ-oxophosphonate with dialkyl phosphites performed on the surface of Al2O3 The adducts revealed unexpected reactivity in the attempted O-acylation reaction, and provided the corresponding…
Abstract The application of enzyme-based therapies has received significant attention in modern drug development. Lipases are one of the most versatile enzymes that can be used as therapeutic agents in basic skin care and medical treatment related to excessive sebum…
Abstract Pancreatic enzyme replacement therapy (PERT) treats pancreatic insufficiency, causing a lack of digestive enzymes due to pancreatic damage or dysfunction. However, traditional PERT faces challenges such as poor stability and limited efficiency of the enzymes. Lipase from Porcine pancreas (PpL) is…
Absztrakt DNA damage tolerance (DDT) pathways mitigate the effects of DNA damage during replication by rescuing the replication fork stalled at a DNA lesion or other barriers and also repair discontinuities left in the newly replicated DNA. From yeast to mammalian…
Absztrakt Screening of ultra-low-molecular weight ligands (MiniFrags) successfully identified viable chemical starting points for a variety of drug targets. Here we report the electrophilic analogues of MiniFrags that allow the mapping of potential binding sites for covalent inhibitors by biochemical…
Absztrakt Covalent inhibition has been attracting significant attention in drug discovery. Here we present the free energy-based computational modeling of both reversible and irreversible covalent inhibitors. The specific features of reversible inhibition are discussed emphasizing the difference between the two-state…