Synthesis of novel pyrimidine and fused pyrimidine derivatives

4-Amino-2-(benzylthio)-6-(4-methoxyphenyl)pyrimidine-5-carbonitrile (1) was prepared by treatment of s-benzylthiuronium chloride with 2-(4-methoxybenzylidene)malononitrile in ethanolic sodium hydroxide with hydrazine hydrate to afford the hydrazino derivative 2, which was allowed to react with different electrophilic reagents to give the pyrimidine derivatives 3-12. The proclivity of (E)-2-cyano-3-(4-nitrophenyl)acrylamide (13) towards carbon and nitrogen nucleophiles was also investigated. IR, 1H NMR and mass spectra for all the synthesized compounds were discussed. All derived compounds were investigated for anti avian influenza (H5N1) virus activity and compared with zanamivir as control drug. All the synthesized compounds didn’t possess any antiviral activity

Improving the Dielectric Properties of High Density Polyethylene by Incorporating Clay-Nanofiller

Polymer nanocomposites have been used for various important industrial applications. The preparation of high density polyethylene composed with Na-montmorillonite nanofiller using melt compounding method for different concentrations of clay-nano filler of 0%, 2%, 6%, 10%, and 15% has been successfully done. The morphology of the obtained samples was optimized and characterized by scanning electron microscope showing the formation of the polymer nanocomposites. The thermal stability and dielectric properties were measured for the prepared samples. Thermal gravimetric analysis results show that thermal stability in polymer nanocomposites is more than that in the base polymer. It has been shown that the polymer nanocomposites exhibit some very different dielectric characteristics when compared to the base polymer. The dielectric breakdown strength is enhanced by the addition of clay-nano filler. The dielectric constant (εr) and dissipation factor (Tan δ) have been studied in the frequency range 200 Hz to 2 MHz at room temperature indicating that enhancements have been occurred in εr and Tan δ by the addition of clay-nano filler in the polymer material when compared with the pure material

A quality assurance technique for the static multileaf collimator mode based on intrinsic base lines

AbstractThe inspection of the static leaf positions of Multileaf Collimator (MLC) devices is essential for safe radiotherapy deliveries in both static and dynamic modes. The purpose of this study was to develop a robust, accurate and generic algorithm to measure the individual static MLC leaf positions. This was performed by extracting leaf tip locations from the radiographic film image and measuring their relative distance from a reference line on the film. The reference line was created with a selected set of MLC leaf sides. The film scaling was created and verified using the physical leaf width. The average measured distance corresponds to a leaf width of 10 mm was 9.95 ± 0.09 mm. The estimated reproducibility of the leaf tips location was ±0.26 mm. The code accuracy was checked by intentionally positioning set of leaves with small errors (1 mm), and the detected deviations from the expected positions ranged from −0.25 mm and +0.32 mm. The algorithm includes two self testing functions in order to detect failures of leaf positioning due to poor film quality and to avoid the potential systematic errors attributable to the improper collimator setting. The code is promising to be more efficient with Gafchromic and Electronic Portal Imaging Device (EPID)

Effect of Watermelon Rind Powder on Gut Microbiome and Weight Loss in Obese Rats

The purpose of this research was to examine the impact of watermelon rind powder on the blood lipid profile of male albino rats (Sprague-Dawley strain), weighing about 200–250 g) were separated randomly into two main groups as follows: The first main group -ve control = 6 rats) was given a basic diet. The second main group (24 rats) was fed a high-fat diet (10% sheep fat) for one month to induce obesity and hypercholesterolemia. Six rats were separated and fed on a high fat diet only as a control (positive group + ve), then the remaining 18 rats were separated into 3 subgroups (6 rats per group). These subgroups 1, 2, and 3 were fed on a basal diet mixed with watermelon rind powder at 5%, 10%, and 15%, respectively. All rats were killed after 8 weeks of experimentation in order to get their blood. LDL, HDL, VLDL, TG, ALT, AST, TC, and HB were determined. Results: Hypercholesterolemia rats fed on a basal diet mixed with watermelon rind powder showed significantly (P<0.05) decreasing liver function enzymes, VLDL, LDL, TC, TG, and VLDL, with significantly (P<0.05) increasing hemoglobin and HDL levels when contrasted with the control groups. Conclusion: Feeding on a basal diet mixed with watermelon rind powder could be utilized as a suitable therapy for obese cases and may lead to microbial diversity

4-Hydroxy-2-methyl-N-(2-thiazole)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide (EX15) and its Cu(II) Complex as New Oxicam Selective Cyclooxygenase-2 Inhibitors

4-Hydroxy-2-methyl-N-(2-thiazole)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide (EX15) as nonsteroidal antiinflammatory drug (NSAIDs) of oxicam family has been synthesized bearing high se-lectivity for cyclooxygenase-2 (COX-2) inhibition and high ability to chelate with Cu(II) ions. The EX15-Cu(II) complex, and [Cu(EX15)(OAc)(H2O)2], were synthesized and characterized by using elemental analysis, spectral (UV-Vis, IR), conductance, thermal and magnetic studies. Two equations were predicted using quantitative structure activity relationship (QSAR) and regression analysis for the COX-2 and COX-1 selectivity (microsomal assay) with a regression correlation (R) close to unity. Two techniques were used to investigate the validity of these equations; macrophage cell line (in vitro) selectivity and collagen-adjuvant arthritis model in rats (in vivo) which showed a significant antioxidant, analgesic and antirheumatic effect for 4-hydroxy-2-methyl-N-(2-thiazole)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide and its Cu(II) complex, [Cu(EX15)(OAc)(H2O)2]. (doi: 10.5562/cca1802

Pathological and physiological studies on the brown rot fungus Monilinia fructicola (Winter) Honey

Call number: LD2668 .T4 1965 E52Master of Scienc

Synthesis and reactions of (Z)-2-imino-5-(3,4,5-trimethoxy benzylidene)thiazolidin-4(H)one

5-Arylmethylene-2-imino-4-oxo-2-thiazolidine 3 was obtained as the sole product from the reaction of α-cyano-3,4,5-trimethoxy cinnamonitrile and/or ethyl-α-cyano-3,4,5-trimethoxy cinnamate (1a,b) with 2-imino-4-oxo-2-thiazolidine 2. The reaction of 3 with benzyl amine gave the imidazolidin-4(H)one derivative 4 while with hydrazine hydrate afforded the dimeric product 5. Also, reaction of thiazolidinone derivative 3 with piperidine gave thiazol-4(5H)one derivative 6 which on treatment with Grignard reagent and active methylene compounds afforded thiazolidin-4-one derivatives 7-9, respectively. Compound 6 was converted to the potassium salt 10 which treated with acetic acid, ethyl chloroacetate and furoyl chloride to give the compounds 11-13, respectively. The structures of all new compounds were evidenced by microanalytical data and spectral data

Induciranje pluripotentnih matičnih stanica upotrebom mRNA: učinak valproične kiseline, 5-azacitidina i askorbinske kiseline

In the bourgeoning fields of tissue engineering and regenerative medicine, induced pluripotent stem cells (iPSCs) technology with gene therapy are promising candidates for alternative stem cell source and cell transplantation. In this study, small molecules as anti-oxidant; ascorbic acid (ASA), histone deacetylase inhibitors (HDACi); Valproic acid (VPA), and DNA methyltransferase inhibitors (DNMTi); 5-Azacytidine (5-AzaC) were examined during the generation of murine iPSCs using mRNA of Yamanaka factors from mouse embryonic fibroblasts (MEFs). These modulators were selected based on their well-known effect on the epigenetic status and chromatin modification during early reprogramming. iPSC generation was performed by using synthesized mRNAs of Yamanaka factors Oct4, Sox2, c-Myc, and Klf4 (OSCK) as a standard reprogramming strategy. Both morphological changes and the expression level of the pluripotency markers were examined. 5-AzaC with 1 μM concentration has a slightly toxic effect on the cells, affecting its proliferation and growing efficiency. In contrast, the use of VPA or ASA led to a two-fold increase in the number of iPSC colonies. The iPSCs cultured with the addition of VPA or ASA showed a high expression of the tested pluripotency markers, with a significant increase, more than that of the cells cultured with the addition of 5-AzaC. These findings shed light on the role of ASA, VPA, and 5-AzaC during murine iPSCs generation using a mRNA reprogramming strategy.Ubrzani razvoj u područjima tkivnog inženjerstva i regenerativne medicine, potaknuo je tehnologiju pluripotentnih matičnih stanica (iPSCs) koja zajedno s genskom terapijom predstavlja obečavajući izvor matičnih odnosno transplantacijskih stanica. U ovom su radu, za vrijeme stvaranja mišjih iPSC-a upotrebom mRNA Yamanaka faktora od mišjih embrionalnih fibroblasta (MEF), istraženi učinci različitih modulatora: malih molekula kao antioksidansa, askorbinske kiseline (ASA), inhibitora histonske deacetilaze (HDACi), valproične kiseline (VPA), inhibitora DNA metiltransferaze (DNMTi) i 5-azacitidina (5-AzaC). Ovi su modulatori odabrani zbog njihova dobro poznatog učinka na epigenetski status i modifikaciju kromatina za vrijeme ranog reprogramiranja. Stvaranje iPSC-a postignuto je upotrebom sintetiziranih mRNA Yamanaka faktora Oct4, Sox2, c-Myc i Klf4 (OSCK). Istražene su i morfološke promjene i razina ekspresije markera pluripotencije. 5-AzaC s koncentracijom od 1 μM imao je mali toksičan učinak na stanice, utječući na proliferaciju i njihov rast. Nasuprot tome, upotreba VPA-a ili ASA-e dovela je do dvostrukog povećanja broja iPSC kolonija. iPSC kultura s dodatkom VPA-a ili ASA-e pokazala je visoku ekspresiju testiranih markera pluripotencije, sa znakovitim višom razinom u odnosu na stanice kojima je dodan 5-AzaC. Ovi rezultati rasvjetljuju ulogu ASA-e, VPA-a i 5-AzaC-a za vrijeme stvaranja mišjih iPSC-a primjenom strategije reprogramiranja mRNA