WATER UPTAKE INTO STRATUM CORNEUM; PARTITION BETWEEN LIPIDS AND PROTEINS

Water uptake in natural and reaggregated stratum corneum was determined by weight difference after storage in an atmosphere of controlled relative humidity.

Interlayer spacing in separated lipids as a function of their water content was determined by low-angle X-ray diffractometry. These values were used as a calibration curve to determine the water content of the lipid bilayers in reaggregated stratum corneum.

The results revealed different behavior of the lipid models compared to natural lipids of the stratum corneum. The additional water taken up after reaggregation of equilibrated lipids and proteins, was equally partitioned between the protein and the natural lipid fraction, while the models gave a proportionally higher water uptake into the lipids at high relative humidity. It is obvious that the models, so far, do not mimic all the properties of the natural stratum corneum lipids.     

Synthesis of Some New Benzopyranopyrimidin-2-Thiol Derivatives

Reaction of 2-mercapto-4-hydroxy-5H-[1]-benzopyrano-[4,3- d ]-pyrimidin-5-one ( 3 ) with phenyl isothiocyanate and methyl acrylate yielded the corresponding 2-(substituted)thio-4-hydroxy-5H-[1]-benzopyrano-[4,3- d ]-pyrimidin-5-ones ( 4 , 5 ). Hydrolysis and hydrazinolysis of 5 gave acid derivative 6 , and hydrazone 7 . Treatment of hydrazone 7 with ethyl acetoacetate, diethyl malonate, and phenyl isothiocyanate yielded the corresponding 2-(substituted)thio-4-hydroxy-5H-[1]-benzopyrano- [4,3- d ]-pyrimidin-5-ones ( 8 , 9 , and 11 ). Cyclization of 11 with 2 N NaOH led to 12 .     

SYNTHESIS OF SPIRO [1,3-BENZODIOXOLE-2,4′-(3′H) QUINAZOLINES]

Abstract

In the present investigation, the authors could obtain a new series of spiranes (1) through the reaction of the high potential quinone tetrachloro-o-benzoquinone with 2-aryl-3-phenyl-3H-quinazoline-4-thiones. Thus, 2,3-diphenyl- (2a), 2-p-tolyl-3-phenyl- (2b) and 2-p-anisyl-3-phenyl- (2c)-3H-quinazoline-4-thiones react readily with tetrachloro-o-benzoquinone, in boiling toluene, to give the corresponding spiro-1,3-benzodioxole-2,4′-(3′H)-quinazolines (1a-c), respectively.     

SYNTHESIS AND BIOLOGICAL ACTIVITY OF SOME NEW 8-HYDROXYQUINOLINE SULPHONAMIDE DERIVATIVES

Abstract

Some new derivatives containing both 8-hydroxyquinoline and sulphonylamino β-lactams and thiazolidinones have been prepared. These compounds were synthesized from the corresponding 8-hydroxyquinoline sulphonylhydrazide (1) by converting it to hydrazones (2). The latter hydrazones (2) were easily transformed to β-lactams (3) and thiazolidinones (4) by cyclocondensation reaction with chloroacetyl chloride and/or mercaptoacetic acid. Some metal chelates with Fe³⁺. Co²⁺+, Ni²⁺, Cu²⁺ and Cd²⁺ have been prepared for some of the compounds and screened in vitro for their biological activity.     

Synthesis and spectroscopic characterization of indomethacin-Cd(II), Ce(III), and Th(IV) complexes: IR, 1H NMR,thermal, and biological studies

Solid complexes have been prepared and characterized by IR, UV-Vis, elemental analysis, and ¹H NMR. Indomethacin forms complexes with Cd(II), Ce(III), and Th(IV) ions in molar ratios (ligand: metal) (2: 1), (3: 1), and (4: 1), respectively. The IR spectra of the complexes suggest that the Indomethacin behaves as a monobasic monodentate ligand coordinated to the metal ions via the deprotonated carboxylate group. Prepared complexes exhibit higher antimicrobial activity against several microorganisms, compared to free ligand.     

Mixed-Isotope Labeling with LC-IMS-MS for Characterization of Protein–Protein Interactions by Chemical Cross-Linking

Chemical cross-linking of proteins followed by proteolysis and mass spectrometric analysis of the resulting cross-linked peptides provides powerful insight into the quaternary structure of protein complexes. Mixed-isotope cross-linking (a method for distinguishing intermolecular cross-links) was coupled with liquid chromatography, ion mobility spectrometry and mass spectrometry (LC-IMS-MS) to provide an additional separation dimension to the traditional cross-linking approach. This method produced multiplet m/z peaks that are aligned in the IMS drift time dimension and serve as signatures of intermolecular cross-linked peptides. We developed an informatics tool to use the amino acid sequence information inherent in the multiplet spacing for accurate identification of the cross-linked peptides. Because of the separation of cross-linked and non-cross-linked peptides in drift time, our LC-IMS-MS approach was able to confidently detect more intermolecular cross-linked peptides than LC-MS alone.