On the basis of known coumarin-based prodrug system, a novel coumarin-based mutual prodrug of 5-fluorouracil and dichloroacetic acid was designed, synthesized and evaluated as a promising oral chemotherapeutic agent basing on in vitro stability study in HCl buffer (pH 1.2) and in phosphate buffer (pH 7.4), as well as in vitro release study in human serum. The chemical structure of prodrug was confirmed by analyzing its FTIR, 1H NMR, 13C NMR and MS-ESI spectra. The results of in vitro kinetic study indicated that the prodrug was significantly stable in HCl and in phosphate buffers, and was hydrolyzed in human serum followed pseudo first order kinetics.
Keywords: Coumarin-bas
... Show MoreNew schiff bases series (VIII) a-e and 1,3-thiazolidin-4-one derivatives (IX) a-e containing the 1,2,4-triazole and 1,3,4-thiazazole rings were synthesized and screening their biological activities. These compounds were identified via Fourier transform infrared (FT-IR) spectra, some via Proton nuclear magnetic resonance (1H-NMR) and mass spectra. The biological results indicated that all of these compounds did not reveal antibacterial effectiveness against (Escherichia coli and Klebsiella species) (G-). Some of these compounds showed moderate antibacterial activity against (Staphylococcus aureus, and Staphylococcus epidermidis) (G+), and all compounds exhibited moderate activity against Candida albicans.
The reaction of starting materials (L-asCl2):bis[O,O-2,3;O,O-5,6-(chloro(carboxylic) methylidene)]- -L-ascorbic acid] with glycine gives new product bis[O,O-2,3,O,O-5,6-(N,O-di carboxylic methylidene N-glycine)-L-ascorbic acid] (L-as-gly) which is isolated and characterized by, Mass spectrum UV-visible and Fourier transform infrared spectrophotometer (FT-IR) . The reaction of the (L-as-gly) with M+2; Co(II) Ni(II) Cu(II) and Zn(II) has been characterized by FT- IR , Uv-Visible , electrical conductivity, magnetic susceptibility methods and atomic absorption and molar ratio . The analysis showed that the ligand coordinate with metal ions through mono dentate carboxylic resulting in six-coordinated with Co(II) Ni(II) Cu(II) ions while with
... Show MoreIn this rescrch,new mixed ligand Schiff base complexes of Mn(II),Co(II),Ni(II),Cu(II), Cd(II), and Hg(II) are formulated from the Schiff base( L)resulting from o-phathalaldehyde(o-PA) with p-nitroaniline(p-NA)as a primary ligand and anthranilic acid as a subordinate ligand. Diagnosis of prepared Ligand and its complexes is done by spectral methods mass spectrometer;1H -NMR for ligand Schiff base FTIR, UV-Vis, molar conductance, elemental microanalyses, atomic absoption and magnetic susceptibility. The analytical studies for the all new complexes have shown octahedral geometries. The study of organicperformance of ligand Schiff base and its complexes show various activity agansit four type of bactria two gram (+) and two gram (-) .
Non-Small Cell Lung Cancer (NSCLC) accounts for about 84% of all lung cancer types diagnosed so far. Every year, regardless of gender, the NSCLC targets many communities worldwide. 5-Fluorouracil (5-FU) is a uracil-analog anticancer compound. This drug tends to annihilate multiple tumour cells. But 5-FU's most significant obstacle is that it gets very easily metabolized in the blood, which eventually leads to lower anticancer activity. Therfore a perfect drug delivery system is needed to overcome all the associated challenges.
In this experiment, an attempt was made to prepare 5-FU loaded poly lactic-co-glycolic acid nanoparticles using solvent evaporation method and subsequently observed the effect of molecular weight of poly l
... Show MoreObjective: Conventional approaches for disinfection, including spraying and immersion, resulted in only surface disinfection of impressions. As a result, self-disinfecting impression materials incorporated with antimicrobial compounds require more extensive studies. The incorporation of a disinfectant into irreversible hydrocolloid impression materials could eliminate the need for the disinfection step by conventional approaches, including spraying and immersion which only result in surface disinfection of impressions. The study was aimed to investigate the effect of incorporation of hypochlorous acid in irreversible hydrocolloid materials on antimicrobial efficiency, detail reproduction, and dimensional stability. Materials and
... Show MoreThe unprejudiced of this education is to gauge the ability of the retinoic acid to induce apoptotic cell death in hematological tumors through caspase dependent or independent apoptotic pathway, The cytotoxicity effects of retinoic acid of different concentrations (400,350,300,250,200,150,100,50,25,12.5 μg\ml) and exposure for all hematological malignancy cell lines (Human non-Hodgkin lymphoma SR and human multiple myeloma (COLO 677) and Human Monocytic Leukemia THP1 and Acute promyelocytic leukemia NB4) have been determined using a microtetrazolium (MTT) assay. Propodeum iodide and alcidine orange (AO/PI) paired discoloration was used to study the ability of retinoic acid to induce apoptosis in the infected cells and examined under fluore
... Show MoreVarious of 2,5- disubstituted 1,3,4-oxadiazole (Schiff base, ?- lactam and azo) were synthesized from 2,5-di (4,4?-amino-1,3,4-oxadiazole which usequently synth-esized from mixture of 4- amino benzoic acid and hydrazine arch of polyphosphorus acid. The synthesized compounds were cherecterized by using some spectral data (UV, FT-IR , and 1H-NMR)