Till now, isatin derivatives have received a lot of interest in organic and medicinal chemistry due to their significant biological and pharmacological activities. Schiff’s and Mannich bases of isatins are an effective group of heterocyclic derivatives that play a significant role in medicinal chemistry as antimicrobial agents. In light of these facts, new Schiff bases and Mannich bases of isatin were synthesized. The monomer Mannich bases; 3(a-e) have been synthesized by reacting isatin with different secondary amines, piperidine, morpholine, and pyrrolidine, dimethylamine, diphenylamine, separately, and formaldehyde, while the dimer (5) formed by using piperazine and formaldehyde which then react separately with Phenylhydrazine to form new Schiff bases 4(a-e), and dimer Schiff base (6) as final products. The structures of the newly synthesized compounds were identified using two spectroscopic methods; (Fourier- transform infrared) FTIR and proton nuclear magnetic resonance spectroscopy (¹H-NMR) analysis. The preliminary in vitro antibacterial and antifungal screening results of new isatin derivatives [4(a-e) and 6] reported moderate to potent antimicrobial activity, the compound 4c exhibited moderate broad-spectrum antibacterial and antifungal activities compared to other derivatives. Moreover, compounds 4c and 6 have a good inhibitory effect against B. subtilis while amoxicillin (standard drug) shows no activity. For antifungal activity compounds (4a-c and 4e) have considerable activity towards C. albicans, whereas compound 4d exhibits slight activity and 6 of no activity.
The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon)
Here, a high sensitive method for biomarker identification according to nanostructure, using enzyme-linked immunosorbent assays (ELISAs), called Nano-ELISA, was presented. Different shapes of gold nanostructures (star and sphere; GNSs and GNPs) with a particle size of 40 nm for sphere particles were altered with a monoclonal antibody (Ab) as a detector Ab. To amplify the optical signal, gold nanostructures were employed as carriers of the signaling specific antibody against insulin growth factor binding protein- 3 (IGFBP-3). The substrate was catalytically oxidized by the Horseradish Peroxidase (HRP) conjugated gold nanostructure, and HRP also enhanced the optical signals, reflecting the amount of the targeting IGFBP-3. In comparison to t
... Show MoreIn the present study, mixed ligand compounds of Mn(II), Ni(II), Co(II), Cu(II), Cd(II) and Hg(II) were synthesized using new Ligand N1,N4-bis (pyrimidin-2-ylcarbamothioyl) succinimide (NPS) derived from [Butanedioyl diisothiocyanate with 2- aminipyridine] as first ligand, proline (pro) as second ligand and evaluation of their antioxidant activities for ligand, nickel and cobalt complex towards 1.1-Di-phenyl-2picrylhydrazyl (DPPH) will be compared to the standard anti-oxidants (i.e. the ascorbic acid). Those materials that have been prepared provided results are a result of exhibiting different activities of the radical scavenging for all of the compounds. Compounds were observed then confirmed through the Fourier-tra
... Show MoreIn this article, Pb2Ba1.7Sr0.3Ca2Cu3O10+δ superconductor material was synthesized using conventional solid-state reaction method. X-ray diffraction (XRD) analysis demonstrated one dominant phase 2223 and some impurities in the product powder. The strongest peaks in the XRD pattern were successfully indexed assuming a pseudo-tetragonal cell with lattice constants of a = 3.732, b = 3.733 and c = 14.75 Å for a Pb-Based compound. The crystallite size and lattice strain between the layers of the studied compound were estimated using several methods, namely the Scherrer, Williamson-Hall (W.H), sizestrain plot (SSP) and Halder Wagner (H.W) approach. The values of crystallite size, calculated by Scherrer, W.H, SSP and H.W methods, were 89.454077
... Show MoreShatt Al-Hilla branches from the left of Euphrates River, U/S Hindiyah Barrage, Iraq, and extends about 100 km. It branches at the end into Shatt Al-Diwaniya 112 km and Shatt Al-Daghara 64 km. The study aims to evaluate and develop (Hilla-Daghara) rivers system, which is included Shatt Al-Hilla and Shatt Al-Daghara. Fieldwork began from (26 October until December) 2020. M9, S5 devices, and the installed staff gauges were used to measure discharges and water levels, respectively. A one-dimensional model was developed for the study area by HEC-RAS, after calibration and verification by field measurements; the Manning's n of Shatt Al-Daghara is found to be 0.022. Five Scenarios were simulated to study the reach under the cu
... Show MoreThe objective of the study was to develop microneedle (MN) patch, with suitable properties to ensure the delivery of a therapeutic level of lornoxicam (LXM) in a period suitable to replace parenteral administration in patients, especially those who fear needles. The used polymers were cold water-soluble polyvinyl alcohol (PVA) and polyvinylpyrrolidone (PVP) of low molecular weight with PEG 400 as plasticizer and Tween 80 (to enhance the release) using micro molding technique. Patches were studied for needle morphology, drug content, axial fracture force measurement and drug release while the optimized formulas were further subjected to pH measurement, folding endurance, ex vivo permeation study, histopathology study, stability study and
... Show MoreItraconazole (ITZ) is an antifungal drug (BCSII) used for the treatment of local and systemic fungal infections. Furthermore, ITZ used as an antifungal prophylaxis for immunocompromised patients.
The objective of the study is to overcome the two problems of low and pH dependent solubility of ITZ by its preparation as floating microparticles.
Firstly, pH-dependent floating microparticles were prepared using oil in water solvent evaporation method, from which the best one (F7) selected as a best pH-dependent formula with composition of ITZ (200mg),EC (800mg), HPMC 15cps (200mg) and safflower oil (2ml) .Then, F7 was compared with the selected Relatively pH-independent ITZ floating microparticles formula wit
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