Newly 4-amino-1,2,4-triazole-3-thione ring 2 was formed at position six of 2-methylphenol from the reaction of 6-(5-thio1,3,4-oxadiazol-2-yl)-2-methylphenol 1 with hydrazine hydrochloride in the presence of anhydrase sodium acetate. Seven newly fused heterocyclic compounds were synthesized from compound 2. First fused heterocyclic was 6-(6-(3,5-di-tertbutyl-4-hydroxyphenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl)-2-methylphenol 3 synthesized from reaction compound 2 with 3,5-di-tert-butyl-4-hydroxybenzoic acid in POCl3. Reaction compound 2 with bromophencylbromide afford 6-(6-(4-bromophenyl)-5H-[1,2,4]triazolo[3,4-b][1,3,4]-thiadiazin-3-yl)-2-methylphenol 4. 6-(6-thio-1,7a-dihydro-[1,2,4] triazolo[3,4-b][1,3,4]-thiadiazol-3-yl)-2-methylphenol 5 was synthesized from reaction compound 2 with CS2 in alkaline ethanolic solution. 6-(6-amino-1,7a-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]-thiadiazol-3-yl)-2-methylphenol 6 was synthesized from cyclization of 2 with cyanogen bromide at room temperature. Compounds 7a-c were synthesized from reaction compound 2 with arylisothiocyanate in dimethyl formamide. The antioxidant ability of these compounds was screened by 2,2-diphenyl1-picrylhydrazyl radical assay (DPPH) and Ferric ion reducing antioxidant power assay (FRAP) assays. Compound 2 and 3 exhibited highest DPPH inhibition and FRAP value compared to rest synthesized compounds. The molecular docking studies of the newly synthesized compounds were screened for their A tubulin binding affinity with the aid of docking studies via MOE 2015. Compounds 4, 7a, 7b and 7c exhibited interaction compared with colchicine reference as potent tubulin inhibitor.
A new set of metal complexes by the general formula [M(P)2(H2O)2]Cl2 has been prepared through the interaction of the new Ligand [N1, N4-bis(4-methoxyphenyl)succinamide] (P) derived from succinyl chloride with p-anisidine with the transition metal ions [Cu(II), Mn(II), Cd(II), Co(II) and Ni(II)]. Compounds diagnosed by TGA, 1 H, 13CNMR and Mass spectra (for (P)), Fourier-transform infrared and Electronic spectrum, Magnetic measurement, molar conduct, (%M, %C, %H, %N). These measurements indicate that (P) is associated with the metal ion in a bi-dentate fashion by nitrogen atoms (the amide group), and the octahedral composition of these complexes is suggested. Staphylococcus Aureus (+) and Escherichia Coli (–) were studied for the antibact
... Show MoreBackground: Simvastatin (SIM) is a lipid-lowering agent to prevent disorders caused by clogged blood vessels. Because of its low solubility, it has low bioavailability. The adsorption technique is effective in improving drug solubility and dissolution rate. Objective: To use magnesium aluminum silicate (MAS) as an adsorbent in combination with Soluplus® as a hydrophilic polymer to formulate SIM as immediate-release tablets (IRTs). Methods: We used the solvent evaporation method to make MAS-loaded SIM in the presence of Soluplus®, making sure that the ratio of SIM to MAS to SOLU was 1:6:3. We then used this mixture to make IRTs. Using the direct compression method, we made all of the SIM-IRT formulas. We used diluents like Avicel
... Show MoreAbstract Background: Acute myeloid leukemia (AML) results from sequential genetic alterations in a normal hematopoietic stem cell or its progenitors giving rise to an autonomous clone that dominates the bone marrow leading to marrow failure. MicroRNAs are short non-coding nucleic acid sequences that regulate post-transcriptional gene expression by base-pairing with their target mRNAs. MiRNAs can be secreted into extracellular fluids and carried to target cells by vesicles or bound to proteins. Intracellular and circulating miRNAs are believed to be useful markers in the diagnosis, prognosis, and treatment of various cancers. Practically, circulating miRNAs are more stable at room temperatures and extreme conditions. Purpose: This study aim
... Show MoreThe study aimed to compare the expression of miR-126-3p and miR-423-5p in patients and normal subjects, and correlate their expression with response to induction therapy. Circulating miR-126-3p and miR-423-5p were measured in the plasma of 43 adult AML patients and 35 age- and sex-matched controls by real time PCR. The foldchange in differential expression for each gene was calculated using the comparative cycle threshold (CT) method (also known as the 2−CT method). For statistical purposes, the fold change was calculated using DDCT (or 2–∆∆Ct) method to find the relative expression of miRNAs. The expression fold change of miR-126-3p was 1.73-fold increase in patients than controls (p= 0.010). The expression fold change of miR-423-5
... Show MoreColorectal cancer (CRC) is the most common disease and cause of death globally. The aim of the study is investigation and detection of some bacterial interfering with CRC occurrence and progression. The study conducted between September 2022 till February 2023, a total of 50 specimens were collected from confirmed CRC patients. In addition, 50 stool specimens were collected from Healthy volunteers, considers as control group. Isolation and identification of bacteria in all collected specimens were done by using cultural and differential media (blood agar, macconkey agar and Pfizer agar), as well as the VITEK- 2 compact system. The bacterial species, in the specimens of control were ( Escherichia coli 50 (86.20%), Klebsiella Pneumoni
... Show MoreThe various properties of the ground and excited electronic states of coumarins 102 using density functional theory (DFT) and time-dependent density functional theory (TDDFT) was calculated by the B3LYP density functional model with 6-31G(d,p) basis set by Gaussian 09 W program. Spectral characteristics of coumarin102 have been probed into by methods of experimental UV-visible, and quantum chemistry. The UV spectrum was measured in methanol. The optimized structures, total energies, electronic states (HOMO- LUMO), energy gap, ionization potentials, electron affinities, chemical potential, global hardness, softness, global electrophilictity, and dipole moment were measured. We find good agreement between experimental data of UV spectrum and
... Show MoreAll major organs may be impacted by the connective disease systemic lupus erythematosus, a separate risk factor for coronary artery disease (CAD). Adhesion molecules like intercellular adhesion molecules (ICAM) and vascular cell adhesion molecules (VCAM) can detect endothelial damage and dysfunction, which appear to play a crucial role. This study investigated whether people with SLE had elevated subclinical and clinical atherosclerosis risk factors. Traditional CAD risk factors such as smoking, hypertension, and hyperlipidemia cannot entirely explain this elevation. It is thought that immunological dysfunction also increases CAD risk in SLE patients. The study aimed to assess early endothelial changes in SLE Iraqi female patients w
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