Reducing of ethyl 4-((2-hydroxy-3-methoxybenzylidene)amino)benzoate (1) afford ethyl 4-((2-hydroxy-3-methoxybenzyl) amino)benzoate (2). Reaction of this compound with Vilsmeier reagent affords novel 2-chloro-[1,3] benzoxazine ring (3). The corresponding acid hydrazide of compound 3 was synthesized from reaction of compound (3) with hydrazine hydrate. Newly series of hydrazones(5a–i) were synthesized from reaction of acid hydrazide with various aryl aldehydes. Antibacterial activity of the hydrazones wassecerned utilizing gram-negative and gram-positive bacteria. Compound (5b) and (5c) exhibited significant antibacterial ability against both gram-negative and gram-positive bacteria, while the compounds(5a) showed mild antibacterial activity. Compounds (5d–i) did not display notable activity. The molecular docking of synthesised compounds were tested inside the pocket of bacterial gyrase enzyme target site by using MOE 2015 software, which acts as Adenosine triphosphate (ATP)-binding domain bacterial gyrase enzyme pocket and novobiocin was used as reference.
5-Fluorouracil is one of the commonly used chemotherapy drugs in anticancer therapy; unfortunately treatment with 5-FU by solely has many drawbacks low lipophilicity, low permeability, low molecular weight, and its relatively poor plasma protein binding; also a brief half-life therefore frequent administration is required to maintain the optimal therapeutic plasma level which in addition to its poor selectivity, drug resistance and limited penetration to cancer cells; leads to increased incidence of side-effects to healthy cells/tissues and low response rates. In order to minimize these drawbacks; 5-FU was chemically conjugated with pyrrolidine dithiocarbamate (PDTC) in a mutual prodrug moiety (S-(9H-purin-6-yl) 3-(
... Show MoreAbstract Background: Kaposi’s sarcoma (KS) is an angioproliferative neoplastic disorder that occurs in different epidemiological forms. Human Herpesvirus type 8 (HHV-8) is established as a causative agent of KS that has been mentioned in textbooks and literature. In the last two decades, KS cases were up searched through many Iraqi medical researches which have been published, but unfortunately, none of which had confirmed this association. Objectives: To assess the association of latent nuclear antigen-1(LANA-1) of HHV-8 among KS patients with clinicopathological parameters and to evaluate if this procedure is valuable for diagnosing this disease through the first immunohistochemical study in Iraq. Methods: This is a clinico-immunohis
... Show MoreThe synthesized ligand [4-chloro-5-(N-(5,5-dimethyl-3-oxocyclohex-1-en-1-yl)sulfamoyl)-2-((furan-2-ylmethyl)amino)benzoic acid] (H2L1) was identified utilizing Fourier transform infrared spectroscopy (FT-IR), 1 H, 13 C – NMR, (C.H.N), Mass spectra, UVVis methods based on spectroscopy. To detect mixed ligand complexes, analytical and spectroscopic approaches such as micro-analysis, conductance, UV-Visible, magnetic susceptibility, and FT-IR spectra were utilized. Its mixed ligand complexes [M(L1)(Q)Cl2] [ where M= Co(II), Ni(II) , and Cd(II)] and complexes [Pd(L1)(Q)] and [Pt(L1)(Q)Cl2]; [H2L1] =β-enaminone ligand =L1 and Q= 8-Hydroxyquinoline = L2]. The results showed that the complexes were synthesised utilizing the molar ratio M: L1
... Show MoreOxazepine [1] is non – nomologous seven –member ring that contain two netroatoms (oxygen and nitrogen ). Meanwhile diazepine [2] contains to nitrogen atoms in seven – member ring.
Diazepam (valium) [3] is used to relive anxiety tension associated with anxiety disorder and muscle spasms (1, 2, 3
... Show MoreBackground: The synthesis and characterization of novel liquid crystalline compounds have garnered signi|cant attention due to their potential applications in biomedical sciences, including drug delivery systems, biosensing, and diagnostic tools. This study focuses on synthesizing and characterizing new thiazolothiadiazole-based liquid crystals and evaluating their mesophase properties. Methods: A series of novel compounds containing 5H-thiazolo[4,3−b][1,3,4] thiadiazole units were synthesized via multi-step chemical reactions. The synthesis involved the reaction of chloroethyl acetate with 4−hydroxybenzaldehyde to yield an aldehyde intermediate, followed by subsequent transformations using hydrazine hydrate, ethylacetoacetate, and 1,2
... Show MoreBackground: A great dental and biomedical interest had been paid to silver nanoparticles because of their antimicrobial activity. Objective: To evaluate the antimicrobial and cytotoxic activity of a newly developed Nano-silver fluoride that was synthesized from moringa oleifera leaf extract against S. mutants. Material and method: The green synthesis method was used to prepare Nano-silver fluoride from moringa oleifera leaf extract. The minimum inhibitory concentration and the minimum bactericidal concentration were evaluated using brain heart infusion plates, while the cytotoxicity was evaluated by the hemolytic activity. Results: Nano-silver fluoride had a bactericidal and bacteriostatic effect (MIC was 60 ppm a
... Show MoreIsatin (1H-indole-2, 3-dione) and its analogs are an important class of heterocyclic compounds. N-benzyl isatins and Schiff bases of isatin analogs have been reported to demonstrate a variety of biological activities. This work illustrates the synthesis of new N-benzylisatin Schiff bases and studies their biological activity. Firstly, Isatin and its analogs; 5-methoxyisatin, 5-fluoroisatin reacted with benzyl iodide to obtain N-benzylated derivatives of isatins 2 (ac). Secondly, these compounds were reacted with different amines (sulphanilamide and 4-methyl sulphonyl aniline) separately, to obtain Schiff bases compounds 3 (ac) and 4 (ac), respectively. The synthesized compounds were characterized by using FT-IR and 1HNMR spectroscopy. The s
... Show MoreIn this research, the preparation of bidentate Schiff base was carried out via the condensation reaction of both the salicylaldehyde with 1-phenyl-2,3-dimethyl-4-amino-5-oxo-pyrazole to form the ligand (L). The mentioned ligand was used to prepare complexes with transition metal ions Mn(II), Co(II), Ni(II), Cu(II) and Zn(II). The resulting complexes were separated and characterized by FTIR and UV-Vis spectroscopic technique. Elemental analysis for Carbon, Hydrogen and Nitrogen elements, electronic spectra of the ligand and complexes were obtained, and the magnetic susceptibility tests were also achieved to measure the dipole moments. The molar conductivities were also measured and determination of chlorine content in the complexes and
... Show MoreAromatic Schiff-bases are known to have antibacterial activity, but most of these compounds are sparingly soluble in water. The present work describes the synthesis of new Schiff-bases derived from branched aminosugars. Treatment of 3-Amino-3-Cyano-3-Deoxy-1,2:5,6-Di-O-Isopropylene-α-D-Allofuranose (1) with the aldehydes (2) under reflux in methanol afforded the Schiff-bases (3) in good yields. The new Schiff-bases were in accord with their NMR, IR spectral data and elemental analysis.