Key words Prins reaction - Friedel–Crafts acylation piperidine schizophrenia

Protein S-acylation is a major posttranslational modification whereby a cysteine thiol is converted to a thioester. A prototype is S-palmitoylation (fatty acylation), in which a protein undergoes acylation with a hydrophobic 16 carbon lipid chain. Although this modification is a well-recognized determinant of protein function and localization, current techniques to study cellular S-acylation ar...

Organocatalytic regioselective acylation of mono- and disaccaharides with various functionalized acid anhydrides has been developed. Acylation of octyl beta-D-glucopyranoside with acid anhydrides derived from alpha-amino acids, cinnamic acid, and gallic acid took place at C(4)-OH with 67-94% regioselectivity in the presence of catalyst 1. Regioselective acylation of disaccharides with functiona...

In conclusion, our results show that inhibitors of acylation may be developed on the basis of analogues of myristic acid. Such inhibitors inhibit not only the N-myristoyl transferase activity, but also acylation of proteins in intact cells. They are also able to inhibit virus acylation. Preliminary results show that they inhibit HIV release from infected H9 cells in culture and therefore may be...

Ras proteins play vital roles in numerous biological processes and Ras mutations are found in many human tumors. Understanding how Ras proteins are regulated is important for elucidating cell signaling pathways and identifying new targets for treating human diseases. Here we report that one of the K-Ras splice variants, K-Ras4a, is subject to lysine fatty acylation, a previously under-studied p...

Protein S-acylation, the reversible covalent fatty-acid modification of cysteine residues, has emerged as a dynamic posttranslational modification (PTM) that controls the diversity, life cycle, and physiological function of numerous ligand- and voltage-gated ion channels. S-acylation is enzymatically mediated by a diverse family of acyltransferases (zDHHCs) and is reversed by acylthioesterases....

Catalysis of the acylation aniline with 3-­hydroxy-2-naphthoic, 1-hydroxy-2-naphthoic, 2-hydroxy-1-naphthoic and 1-hydroxy-4-naphthoic acids by phosphorus P(III) silicon Si(IV) compounds leads to formation anilides corresponding hydroxy­naphthoic under mild conditions (ortho-xylene, 146.5–147 °C) in almost quantitative yield.
 Among trichloride tribromide; phosphorous, 1-hydroxyethyli­de­n...

The catalytic preparation of substituted benzanilides by the reaction benzoic acids with aniline is an important model process that has been intensively deve­lo­ped recently, in field «green chemistry» concept, direct amidation, and its study urgent scientific practical task.
 Within framework solving this problem, catalysis acylation trivalent phosphorus compounds P(III) was studied. It e...

2D NMR revealed a correspondence between the molecular structure of lignins and their degree of acylation in several nonwoody angiosperms characterized by different lignin acylation types (acetate and/or p-coumarate esters) and extents (up to more that 90% of units). Some of the lignin substructures identified showed that acylation is produced at the monolignol level. Direct evidence was also p...

Protein S-acylation, the only fully reversible posttranslational lipid modification of proteins, is emerging as a ubiquitous mechanism to control the properties and function of a diverse array of proteins and consequently physiological processes. S-acylation results from the enzymatic addition of long-chain lipids, most typically palmitate, onto intracellular cysteine residues of soluble and tr...