Shahidine, a novel and highly labile oxazoline from Aegle marmelos: the parent compound of aegeline and related amides

A rare alkaloid, shahidine (1), having an unstable oxazoline core has been isolated as a major constituent from the fresh leaves of Aegle marmelos. It is moisture-sensitive, and found to be the parent compound of aegeline and other amides, however, it is stable in dimethyl sulfoxide. Its structure was established by spectroscopic analysis. Biogenetically, oxazolines may be considered as the precursor of hydroxy amides and oxazoles found in plants. Shahidine (1) showed activity against a few Gram-positive bacteria.     

Studies on the kinetics of growth of silver nanoparticles in different surfactant solutions

We produced gels using electrolytic-reduction ion water and magnesium aluminum silicates (smectone^®), and evaluated in detail gel properties in the presence of various types of salt (NaCl, KCl, CaCl₂, MgCl₂, and AlCl₃). Each salt was added to deionized-distilled water or electrolytic-reduction ion water, and phase diagrams for the smectone^® concentration (2.0–4.0%) were produced. The areas of the three phases of smectone^® (gel, sol, and separation) at each salt concentration were expressed as percentages of the total area. As a result, uni- and polyvalent cations (excluding Ca²⁺ ions) affected the stability of gels produced using electrolytic-reduction ion water, and, particularly, univalent cations (Na⁺, K⁺) markedly improved gel stability.Using electrolytic-reduction ion water as a dispersal medium, drug delivery systems (DDS) that can maintain the gelling state can be prepared. Thus, gel preparations with maintained functions or controlled-release transdermal drugs can be obtained.     

Synthesis and antimicrobial evaluation of some 1,3-thiazole, 1,3,4-thiadiazole, 1,2,4-triazole, and 1,2,4-triazolo[3,4-b][1,3,4]-thiadiazine derivatives including a 5-(benzofuran-2-yl)-1-phenylpyrazole moiety

Abstract  

Potassium hydrazinecarbodithioate were prepared by treatment of acid hydrazides with carbon disulfide in the presence of potassium hydroxide. Reaction of this potassium salt with hydrazine hydrate, phenacyl bromide, or hydrazonoyl chlorides afforded 1,2,4-triazole, 1,3-thiazole, and 1,3,4-thiadiazoles. Reaction of 1,2,4-triazole with phenacyl bromide or hydrazonoyl chlorides afforded the corresponding 1,2,4-triazolo[3,4-b][1, 3, 4]-thiadiazines. All these new compounds were screened for antibacterial and antifungal activity. Some had promising activity.     

Synthesis,antiviral and antimicrobial screening of some new 2-oxoindoline derivatives

New 3-(2-(5-(aryldiazenyl)-4-methylthiazol-2-yl)hydrazono)indolin-2-ones were prepared by the reaction of isatin β-thiosemicarbazone with different hydrazonoyl chlorides. Imide derivatives were prepared by the reaction of isatin hydrazone with various anhydrides, and a series of new sulfonimides was also synthesized. All new compounds were tested for their biological activities.     

Spectrophotometric Determination of Piroxicam via Chelation with Fe(III) in Commercial Dosage Forms

The objective of this work is to develop and validate spectrophotometric method for the determination of piroxicam in commercial dosage forms. The method is based on the chelation of the drug with Fe(III) to form pink coloured metal chelate at room temperature which absorbs maximally at 504 nm. Beer's law is obeyed over the concentration range of 8–160 μg mL^?1 (A = 1.07 × 10^?3 + 7.75 × 10^?3 C). Under the optimized experimental conditions, proposed method is validated as per the International Conference on Harmonisation guidelines. The limits of detection and quantitation for the proposed method are 0.775 and 2.348 μg mL^?1, respectively. The proposed method has been successfully applied to the determination of piroxicam in commercial dosage forms. The results are compared with the reference El‐Ries et al. spectrophotometric method.     

Anionic clay–Pt metal nanoparticle composite through intercalation of hexachloroplatinate in nickel zinc hydroxysalt

Nickel zinc hydroxysalt–Pt metal nanoparticle composite was prepared by intercalation of the anionic platinum complex, [PtCl₆]^2? in nickel zinc hydroxysalt through ion exchange reaction and subsequent reduction of the platinum complex by ethanol. Powder X-ray diffraction and microscopy studies indicate that the process of reduction of the platinum complex in the interlayer region of the anionic clay takes place topotactically without destroying the layers.     

Kinetic study of the complex reaction between copper(II) and 2-(2′-hydroxy-3′-methoxyphenyl)benzothiazole

2-(2′-Hydroxy-3′-methoxyphenyl)benzothiazole reacts with copper(II) in an ethanol/water mixture to form an O,S chelate which exhibits the remarkable property of changing the chelation site above a pH of ca. 5.0, to the O,N site. The detailed kinetics of this reaction in an ethanol/water mixture (3:1) at a temperature of 25 °C was investigated using a stopped-flow spectrophotometric technique employing a wavelength of 400 nm. The initial complex, Cu(O,S), is formed via a fast, reversible second-order complex formation step whereupon the formation of the Cu (O,N) follows first order kinetics. The Cu(O,N) complex is, however, unstable towards internal electron exchange and after the reaction is complete, a black polymeric material very slowly precipitates out of solution. Rate and equilibrium constants for the postulated reactions are presented and discussed.     

Thermal properties of polylactides

A thermal analysis of a series of polylactides (PLA) was carried out based on the number of average molecular mass (M _n), and the nature of isomer (D, L and DL). It is confirmed that the glass transition temperature (T _g) of PLA increased as a function of molecular mass irrespective of isomer type except sample with a high polydispersity index. The melting temperature (T _m) and enthalpy of crystal fusion (ΔH _f) of L-isomer increased as the M _n was increased from 1100 to 27500. The degree of crystallinity (χ_c%) increased as a function of molecular mass. However no crystallization peak was detected in the lower molecular mass range (550–1400). The non-isothermal crystallization behavior of the PLA melt was significantly influenced by the cooling rate. Both D and L isomers exhibited insignificant difference in thermal properties and DL lactides exhibited amorphous behavior at identical molecular masses. Change in microstructure showed significant difference between two isomers. Analysis of the FTIR spectra of these PLA samples in the range of 1200–1230 cm⁻¹ supported DSC observation on crystallinity.     

Efficient Solid‐Phase Synthesis of Sulfotyrosine Peptides using a Sulfate Protecting‐Group Strategy

Double protection : Efficient Fmoc‐based solid‐phase synthesis (SPPS) of sulfotyrosine (sY) peptides is achieved by incorporating the sY residue(s) as a dichlorovinyl‐protected (DCV) sulfodiester(s) and using 2‐methylpiperidine for Fmoc removal. After removal of the other protecting groups, the DCV group could be cleaved by mild hydrogenolysis giving the sY peptides in good yield.