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Synthesis of Phthalimide Imine Derivatives as a Potential Anticancer Agent
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The outstanding evidence of phthalimide pharmacophore in securing enhanced biological activities had encouraged further research and development into phthalimide-based derivatives as potential new drugs. In this study, phthalimide core was hybridized with aldehydes giving integrated imines displaying different types of functionalities and at alternating positions. The resulting compounds, therefore, provide an innovative window to explore possible differential biological effects as antioxidants and anticancer agents. A total of sixteen compounds were synthesized, and each was verified by FT-IR, H NMR, C NMR, and MS characterization. Herein, a facile single-step synthesis method was employed substituting the conventional two-step chemical production routes. Among the sixteen tested compounds, the H7 compound with hydroxyl phenolic group has shown an eminent antioxidant activity with a 19.52% decrease to the IC50 value compared to that of the control standard BHT antioxidant. On the other hand, the halogenated H6 Schiff base structure was successful in securing effective cancer inhibition to both colon and breast cancer cell lines, while maintaining selective action toward normal tissues. Results have collectively indicated the importance and impactful effects of functional groups position and types within similar basic structures, in directing different biological outcomes.

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Application of Seed Mucilage Extracted from Lallemantia royleana as a Suspending Agent
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The mucilage from the seeds of Lallemantia royleana family Labiatae was extracted and subjected to preformulation study for evaluation of its suitability for use as suspending agent. Furosemide suspensions were prepared using (1.5% w/v) of the extracted Lallemantia royleana mucilage, (1.5% w/v) chitosan and (0.35% w/v) xanthan gum. The mucilage was white in color and the average yield of dried mucilage obtained from L.royleana nutlets was 14 % w/w of the seeds used. It is sparingly soluble in water but swells in contact with it, giving a highly viscous solution. It is slightly acidic to neutral. It was found that the extracted natural mucilage of Lallemantia royleana exhibited a higher viscosity profil

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Publication Date
Fri Mar 01 2024
Journal Name
Physical Chemistry Research
Exploring the Potential of Quantum Chemical Calculations for Synthesized Quinazoline Derivatives as Superior Corrosion Inhibitors in Acidic Environment
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Hydrochloric acid (HCl) is a substance that is frequently utilized in industrial operations for important tasks such as chemical cleaning and pickling metallic surfaces.Therefore, the corrosion inhibition ability of three newly synthesized quinazoline derivatives namely, 3-allyl-2-(propylthio) quinazolin-4(3H)-one) (APQ), (3-allyl-2-(allylthio) quinazolin-4(3H)-one) (AAQ), (3-allyl- 2-( Prop -2-yn -1-ylthio) Quinazolin - 4 (3H) - one) (AYQ) were theoretically determined and these compounds were characterized using Fourier Transform Infra-Red (FTIR) and 1H and 13C Nuclear Magnetic Resonance (NMR) spectroscopic. A series of quantum chemical properties of these derivatives: EHOMO, ELUMO, energy gap (ΔE),dipole moment (μ), hardness (η), soft

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Publication Date
Sun Sep 04 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Some New Pyrazoline and Isoxazoline Derivatives as Antibacterial Agents
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In this paper some chalcones (C1-C8) are prepared based on the reaction of one mole of substituted acetophenone with one mole of substituted benzaldehydes in the presence of (40%) sodium hydroxide as a base. Pyrazolines (P1–P8) are prepared from the reaction of chalcones (C1-C8) with hydrazine hydrate. Isoxazoline (I1-I8) is prepared from the reaction of chalcones (C1-C8) with hydroxyl amine hydrochloride in the presence of (10%) sodium hydroxide as a base. These compounds are characterized by using various physical and spectral methods. The compounds are screened for their in vitro antibacterial activity using gram-positive bacteria and gram-negative bacteria. Several derivatives of pyrazolines and isoxazolines are produced well to moder

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Publication Date
Thu Mar 16 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis and Characterization of New Phthalimides Containing 1, 2, 4-triazole and Imine Group
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Several new derivatives of 1, 2, 4-triazoles linked to phthalimide moiety were synthesized through following multisteps. The first step involved preparation of 2, 2-diphthalimidyl ethanoic acid [2] via reaction of two moles of phthalimide with dichloroacetic acid. Treatment of the resulted imide with ethanol in the second step afforded 2, 2-diphthalimidyl ester [3] which inturn was introduced in reaction with hydrazine hydrate in the third step, producing the corresponding hydrazide derivative [4]. The synthesized hydazide was introduced in different synthetic paths including treatment with carbon disulfide in alkaline solution then with hydrazine hydrate to afford the new 1, 2, 4-triazole [10]. Reaction of compound [10] with different alde

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Publication Date
Thu Feb 25 2021
Journal Name
Iraqi Journal Of Agricultural Sciences
ROSEMARY VOLATILE OIL AS A PRESERVATIVE AGENT IN SOME CANNED MEAT FOODS
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This research was aimed to evaluate activity of Rosemary volatile oil and Nisin A in vivo and on B. cereus isolated from some canned meat products in vitro. The results showed that the activity of Rosemary volatile oil (2000 µg/ml) and Nisin A (350 µg\ml) attained to 27 and 19 mm inhibitory zone diameter respectively in well diffusion method. The viable plate count from samples of canned meat treated with effective concentration of Rosemary volatile oil and Nisin A were examined. The samples with Rosemary volatile oil was not showed any CFU/g after 9 days of preservation while sample with Nisin A and control observed 49 and 45 CFU/g respectively. In vivo experiment on mice, two weeks after oral dose of Rosemary volatile oil (2000

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis and Biological Effectiveness of Some new Azo Compounds as Derivatives of Nitrogen Bases
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In this study the new azo compounds (3compounds) for nitrogen bases (Adenine and Cytosine) are synthesized through two reaction steps (formation of diazonium salt and coupling reaction). The compounds have been characterized by FTIR, melting point, and ultra-violate (UV) spectra. All synthesized compounds have been estimated in vitro for their antimicrobial activities against two species of bacteria(E.coli, S.aureus)and one kind of fungi ( Aspergillus flavus) .The results show that these compounds have very good antibacterial and antifungal activities especially compounds 1 and 3.To study the effect of these compounds were making some physiological tests on rats are made ,the results of hematological study showed decreasing level of

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Preliminary Pharmacological Evaluation of New Analogues of Diclofenac as Potential Anti-inflammatory Agents
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         A group of amine derivatives [4-aminobenzenesulfonamide derivatives, 2-aminopyridine and 2-aminothiazole] incorporated to α-carbon of diclofenac a well known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were designed and synthesized for evaluation as  a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of the selected final compounds (9, 12 and 13) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (3 mg/Kg) of diclofenac sodium. All tested compounds  produced a significant reduction  in paw edema with respect to the effect of propylene glycol 50

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Publication Date
Tue Dec 19 2023
Journal Name
Journal Of Madenat Alelem College
Review Article: Amygdalin as Anti-Cancer Agent
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Amygdalin (d-Mandelonitrile 6-O-β-d-glucosido-β-d-glucoside) and its semi synthetic product is Laetrile ( also called vitamin B17): a natural cyanogenic glycoside occurring in the seeds of some edible plants, such as bitter almonds and peaches. Early in the 19th century, Amygdalin was first isolated in 1830 by two French chemists, Robiquet and Boutron-Charlard, as active components in various fruit pits and raw nuts. However, the systematized study of vitamin B17 started when chemist Bohn (1802) discovered that a hydrocyanic acid is released during distillation of the water from bitter almonds. The various pharmacological effects of Laetrile include antiatherogenic, activity in renal fibrosis, pulmonary fibrosis, immune regulation, ant

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Publication Date
Wed Jul 10 2024
Journal Name
Pharmacia
Molecular docking, ADMET, synthesis and evaluation of new indomethacin hydrazide derivatives as antibacterial agents
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Bacterial infections pose an ongoing challenge due to resistance developed by infectious bacteria. So much research targeting designing new antibacterials is published annually. Our goal is to synthesize compounds that have given antibacterial activity according to molecular docking against the chosen target protein and that have acceptable ADMET properties that can be synthesized and used in the future. New 2-(5-methoxy-1-(4-chlorobenzene)-2-methyl-1H-indol-3-yl)acetohydrazide derivatives’ antibacterial efficacy against two common strains of Gram-negative and Gram-positive microorganisms has been developed, produced, and investigated. Sophisticated, modern analytical methods, including ATR-FTIR and 1H NMR spectroscopy, were used

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Publication Date
Tue Oct 22 2019
Journal Name
Scientia Pharmaceutica
Design, Synthesis, and Docking Study of Acyl Thiourea Derivatives as Possible Histone Deacetylase Inhibitors with a Novel Zinc Binding Group
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Histone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with novel zinc binding groups. The present study describes the utilization of acyl thiourea functionality, known to possess the ability to complex with metals, to be a novel zinc binding group incorporated into the designed histone deacetylase inhibitors. N-adipoyl monoanilide thiourea (4) and N-pimeloyl monoanilide thiourea (5) have been synthesized and characterized successfully. They showed inhibition of growth of human colon adenoc

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