Synthesis and Pharmacological Activity of Annelated Pyrimidine Derivatives

A series of 2,3-diglycosylpyrimidine 4, annelated pyrimidine derivatives, pyrazolo-[3,4-d]pyrimidine 8, ditetrazolo[1,5-a; 1′5′]pyrimidine 9, 2,9a,10-triazaanthracene 12, thieno- [2,3-d]pyrimidine 14, 9-thia-1,3,5,7-tetraazafluorene-8-one 15, 7-oxa-9-thia-1,3,5-triazafluorene-8-one 16, and 5-oxa-9-thia-1,3-diazafluorene 21a , b derivatives have been synthesized via a sequence of heterocyclization reactions of suitably functionalized 6-[5-(4-bromophenyl)oxazol-4-yl]-1,2,3,4-tetrahydro-2-thioxo-4-oxopyrimidine-5-carbonitrile (2) with different electrophiles and nucleophiles. The new compounds were prepared with the objective to study their pharmacological properties.     

Novel Syntheses and Reactions of Polynuclear Heterocyclic Derivatives Derived From Thioxopyridopyrimidine,With a New Ring System

Pyridopyrimidine derivatives 2 reacted with hydrazonoylchloride derivatives and yielded triazolopyridopyrimidines 6a–f. Compound 4b reacted with aliphatic acids and afforded triazolo-pyridopyrimidines 7a,b, and the reaction with carbon disulfide afforded 10-mercapto-triazolopyridopyrimidine (10). Moreover, the reaction of 4b with β -ketoesters afforded 10-pyrazolyl-pyridopyrimidines derivatives 11, 13, 14, and 15. Compound 4b reacted with nitrous acid to give tetrazolopyridopyrimidine 16, which reduced to 10-amino-derivative 17. On the other hand, the reaction of 4b with aromatic aldehydes afforded arylidines derivatives 18a–c, which were later cyclized to triazolo-pyridopyrimidines deivatives 19a–c. Finally, 4b reacted with α-haloketones to give triazines derivativrs 20, with new ring systems.     

Manufacturing,thermal stability,and flammability properties of polypropylene containing new single molecule intumescent flame retardant

Melamine salt of pentaerythritol phosphate kaolin (MPPK) was synthesized by the reaction of pentaerythritol phosphate with kaolin (K) and melamine. The structure of MPPK was confirmed by EDXS, ¹H NMR, FTIR, and XRD. MPPK was blended with polypropylene (PP) at different loading levels. Thermogravimetric analysis (TGA) results showed that MPPK improved the thermal stability of PP at high temperatures in all PP composites. Vertical burning rate test manifested that PP composites can achieve V0 at 20% and 25% MPPK loading levels. Cone calorimeter data exhibited that addition of 25% MPPK to PP reduced peak of heat release rate (pHRR) and total heat release (THR) by 86% and 76% and increased the char residue after test to 67%. The results of PP/25% MPPK composite were compared with the data obtained from PP containing 25% K and 25% of traditional intumescent flame retardant composed of melamine phosphate (MP), pentaerythritol (PE), and K. The outcomes indicated that MPPK was more efficient in flame retardancy than the other systems. The digital photographs and SEM images for char residue demonstrated that MPPK succeeded in forming cellular and coherent char layer on the PP surface. The main advantage of adding 25% MPPK to PP was its ability to preserve nearly the inner half of the sample without burning after cone calorimeter test.     

Reactive intermediates in the reaction of hydrazinecarbothioamides with 2-(bis(methylthio)methylene)malononitrile and ethyl 2-cyano-3,3-bis(methylthio)acrylate

Research on Chemical Intermediates - The reaction of N-substituted hydrazinecarbothioamides with both 2-(bis(methylthio)methylene)malononitrile and ethyl 2-cyano-3,3-bis(methylthio)acrylate...     

Quantitative analysis of the low molecular weight serum proteome using 18O stable isotope labeling in a lung tumor xenograft mouse model

With advancements in the analytical technologies and methodologies in proteomics, there is great interest in biomarker discovery in biofluids such as serum and plasma. Current hypotheses suggest that the low molecular weight (LMW) serum proteome possesses an archive of clipped and cleaved protein fragments that may provide insight into disease development. Though these biofluids represent attractive samples from which new and more accurate disease biomarkers may be found, the intrinsic person-to-person variability in these samples complicates their discovery. Mice are one of the most extensively used animal models for studying human disease because they represent a highly controllable experimental model system. In this study, the LMW serum proteome was compared between xenografted tumor-bearing mice and control mice by differential labeling utilizing trypsin-mediated incorporation of the stable isotope of oxygen, 18O. The digestates were combined, fractionated by strong cation exchange chromatography, and analyzed by nanoflow reversed-phase liquid chromatography coupled online with tandem mass spectrometry, resulting in the identification of 6003 proteins identified by at least a single, fully tryptic peptide. Almost 1650 proteins were identified and quantitated by two or more fully tryptic peptides. The methodology adopted in this work provides the means for future quantitative measurements in comparative animal models of disease and in human disease cohorts.     

Adsorption Behaviour of 134Cs and 22Na Ions on Tin and Titanium Ferrocyanides

Tin and titanium ferrocyanides were studied as adsorbents for alkali metal ions, viz., ¹³⁴Cs and ²²Na, which represent radioactive wastes. The ferrocyanides were prepared in granular form. The tin version contained 11.2% water, while the titanium version contained 17.7% water. The exchange capacities for Cs⁺ and Na⁺ in the hydrated tin version were about 1.5 and 0.7 meq/g, respectively, while those in the titanium version were 2.2 and 1.2 meq/g, respectively. Drying at 250°C decimated those capacities. The diffusional time constant of Cs⁺ at 25°C, determined via Fick's second law, was of order of magnitude 1 × 10^–3 s^–1, though there were minor differences due to particle size and the form of ferrocyanide. Similarly, the effective diffusivity was of order of magnitude 1 × 10^–8 cm²/s. The titanium version responded slightly faster than the tin version. Likewise, equilibrium measurements in mixtures with sodium nitrate, potassium nitrate, or uranium oxide, showed that the titanium version exhibited significantly greater selectivity for Cs⁺ than did the tin version. Unfortunately, tests of complete elution of the Cs⁺ from the ferrocyanides were mostly disappointing. Work continues on that subject.     

Novel Synthesis of Pyrazolyloxothiazolidine Derivatives

1‐Substituted 3‐[3‐(methyl/phenyl)‐1H‐pyrazol‐5‐yl]thioureas react with the triple bond of dimethyl acetylenedicarboxylate forming (Z)‐methyl 2‐[(Z)‐3‐substituted‐2‐(3‐(methyl/phenyl‐1H‐pyrazol‐5‐ylimino)‐4‐oxothiazolidin‐5‐ylidene)acetates. Rational for these conversations are presented.     

Effect of some environmental ligands and fertilizers on humic acid complexation with strontium

The effect of some environmental ligands and certain fertilizers on the complexation of strontium with humic acid wasinvestigated colorimetrically and radiometrically. The results indicate that Na₂-EDTA, Na₃-citrate and NaCl compete to complex strontium in solution with the sequence: chloride < citrate < EDTA while Na₃-phosphate has the reverse behavior. In the case of nitrogen containing fertilizers, the results show that urea, Mg-ammonium nitrate and ammonium nitrate increase the availability of strontium to plants and microorganisms.     

Extraction of tungsten and rhenium by basic or neutral extractants in xylene from mineral acidic media

Extraction of WO ₄ ^2– and ReO ₄ ^– by Adogen-381, tricaprylmethylammonium chloride, Hyamine 10-X, trioctylphosphine oxide or dibenzylsulphoxide in xylene from HNO₃, HCl or H₂SO₄ acid medium was investigated. Based on the separation factors obtained, the separation of ReO ₄ ^– from WO ₄ ^2– was elucidated. ReO ₄ ^– was separated from WO ₄ ^2– in high radiochemical purity: >99.9% by three successive extractions and strippings using Adogen-381 from HCl or HNO₃ acid medium.     

New Pyrimidine‐2‐thiones from Reactions of Amidrazonethiols with 2‐Amino‐1,1,2‐ethenetricarbonitrile and Investigation of Their Antitumor Activity

Reactions of thiosemicarbazones with 2‐amino‐1,1,2‐ethenetricarbonitrile were reported. The reaction occurred in the amidrazonyl site, and new pyrimidine‐2‐thiones were obtained. The reaction mechanism was discussed. The structure of products was elucidated by MS, IR, and NMR spectra together with elemental analyses. The antitumor activity was evaluated against one tumor cell line. Using a standard MTT assay, the effect of the samples on the growth of HepG2 cells was investigated. Half of these compounds showed no cytotoxic effect on HepG2 cells, while the others result in decreasing in the HepG2 cell viability.