To investigate the importance of increased hydrophobicity at the amino end of antimicrobial peptides, a dermaseptin derivative was used as a template for a systematic acylation study. Through a gradual increase of the acyl moiety chain length, hydrophobicity was monitored and further modulated by acyl conversion to aminoacyl. The chain lengths of the acyl derivatives correlated with a gradual i...

Post-translational modification of proteins with hydrophobic lipid-derived substituents is increasingly becoming recognized as a major route for targeting proteins to membranes. Glycosylphosphatidylinositol (GPI) anchors are found at the C terminus of a wide range of cell surface proteins, and may endow the cell with the ability to release them in a controlled fashion via specific phospholipase...

Fatty acylation of cysteine residues provides spatial and temporal control of protein function in cells and regulates important biological pathways in eukaryotes. Although recent methods have improved the detection and proteomic analysis of cysteine fatty (S-fatty) acylated proteins, understanding how specific sites and quantitative levels of this posttranslational modification modulate cellula...

In this work we developed C(2)-symmetric chiral nucleophilic catalysts which possess a pyrrolidinopyridine framework as a catalytic site. Some of these organocatalysts effectively promoted asymmetric desymmetrization of meso-diols via enantioselective acylation.

New metal ion complexes of ampicillin were synthesis by two steps, first N-acylation with benzoyl chloride and sebacoyl chloride, In the second step, prepared compounds reacted cupric to form Cu- complexes. FT-IR, 1H NMR, 13C UV- visible, Elemental analysis, and, a theoretical study was used distinguish The biological efficacy compound found more active against bacteria.

an efficient method for the friedel–crafts acylation of a wide range of aromatic compounds in good to excellent yields under solvent-free conditions, using iron zirconium phosphate (zpfe) was investigated. the catalyst is easy to prepare and shows interesting catalytic properties. the catalyst was characterized by some instrumental techniques such as xrd, icp-oes, sem and tem. a wide variety of...

We demonstrated recently that organocatalysts, based on a nucleophilic core (N-alkylimidazole or 4-aminopyridine) and decorated with an extensive secondary-sphere envelope (connected to the through benzyl substituent), strongly affect site selectivity in acylation phosphorylation of amphiphilic diols, sometimes entirely overriding innate predisposition substrate. Preliminary studies pointed out...

quinazolinones are interesting materials because of their valuable biological effects. in this study some new 2,3-disubstituted-4(3h)quinqzolinone derivatives were synthesized from anthranilic acid in six steps by introducing a new chiral center to the aliphatic side chain of the quinazolinone. in the last step, a single acylation on the hydrazine moiety afforded final compounds. the structures...

Of the 4 tyrosyl residues of bovine ar-lactalbumin, 2 were found to be quite reactive with N-acetylimidazole; the third group is less so, and the fourth is only weakly reactive. Acylation of the two most reactive groups results in a reversible increase in the quantum yield of a tryptophan residue or residues which emit maximally at 350 rnp. At relatively high concentrations of reagent, in addit...

Incubation of rat sciatic nerve slices with Krebs-Ringer bicarbonate buffer containing [3H]palmitic acid resulted in the acylation of the PO glycoprotein and a 24 kDa protein of the peripheral nerve myelin. Radioactivity was removed from PO after treating PO with hydroxylamine (83%) and methanolic KOH (97%). These results provided evidence that the radioactivity incorporated into PO was not due...