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Synthesis, molecular docking and anti-inflammatory evaluation of new trisubstituted pyrazoline derivatives bearing benzenesulfonamide moiety
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Publication Date
Wed Oct 04 2023
Journal Name
History Of Medicine
Theoretical Biological Activities and Docking studies of new amino-acids Derivatives of Oseltamivir for The Treatment of Coronavirus Disease 2019
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Antiviral medications may be the best choices for COVID-19 treatment until particular therapeutic treatments become available. Tamiflu (oseltamivir) is a neuraminidase inhibitor licensed for the management and defense against influenza types A and B. Oseltamivir-based medication combinations are currently being used to treat COVID-19 patients who also have the new coronavirus 1 SARS-CoV-2. 1 Oseltamivir administration was related with a less time spent in the hospital, quicker recovery 1 and discharge, and a decreased mortality rate. Docking is a modern computational method for identifying a hit molecule by assessing the binding ability of molecular medicines within the binding target pocket. In this work, we chose 21 ligand compounds that

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Publication Date
Mon Feb 20 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis of Some New 2-thioxoimidazolidin-4-one Derivatives
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This research includes the synthesis of new series of heterocyclic compounds. Reaction of 2-nitro benzylidene)thiosemicarbazide(1) with ethyl chloro acetate gave (2-nitro benzylidene amino)-2-thioxomidazolidine-4-one(2) ,treatment(2) with methyl iodide to give(3)which was reacted with hydrazine to give 2-hydrazinyl-1-[(2-nitrobenzylidene)amino]- 1H-imidazol-5(4H)-one, andreation of compound(2) with aromatic aldehydes to give 5arylidene -3-({2-nitro benzylidene}amino)2-thioxo-3,5-dihydro-4H-imidazole-4-one(5a,5b), which was reacted with ethyl aceto acetate to give 4-aryl-1-[2-nitrobenzylidene, amino -6oxo-2-thioxo octa hydro-1H-benzo[d]imidazole-5-carboxylate and followed synthesis of βlactamederivtives(9a,9b) by treatment derivatives(

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis of New Some Imidazole Derivatives Containing ?-Lactam Ring
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In this work 5-methylene-yl - (2-methy –oxazole-4-one) (1H) imidazole (1) were synthesized from the reaction of L-Histidine with acetic anhydride and which converted to the of 5-methylene-yl-(2-methyl 3-amino imidazole-4-one)-1H-imidazole (2) by reaction with hydrazine hydrate. Schiff bases (3-6) were synthesized from the reaction of compound (2) with different aromatic aldehyde. Reaction of compounds (3-6) with chloroacetyl chloride gives azetidinone one derivatives (7-10). These compounds were characterized by FT-IR and some of them with 1H-NMR and 13C-NMR spectroscopy.

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Publication Date
Thu Mar 16 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis of Some New Heterocyclic Compounds Via Chalcone Derivatives
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  The chalcones 1( a,b) were prepared by the reaction of  2- acetyl benzofuran with two aromatic aldehydes in the presence of alkaline media. These chalcones are used as starting material to obtain the  desired heterocyclic: pyrazolin, isoxazoline, pyrimidinthion, pyrimidinone, cyclohexanone and indazole derivatives. The structure of newly synthesized heterocyclic compounds were established on the basis of  their melting points, elemental analysis(C.H.N), FTIR and 1HMNR (for some of them) spectral data . The synthesized compounds have been screened for their antibacterial activities, they exhibited good antibacterial activity against Escherichia coli (G-) and Staphylococus aureus (G+) . 

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Publication Date
Sat Dec 04 2021
Journal Name
International Journal Of Drug Delivery Technology
Evaluation of the Anti-inflammatory and Anti-oxidant Activity of Crab Components and Crab Shell in Experimental Rats in Comparison with Dexamethasone and Diclofenac Sodium
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Crabs belong to the crustacean family (Decapods crustacean), and their shells contain natural ingredients from which the bioactive compounds are derived. It has been used as folklore medicine in cancer treatment. We investigate the possible anti-inflammatory and anti-oxidant effects for crab shells and whole crabs. Thirty-six rats (150–200 gm) from both sexes were used, divided into six groups, the anti-inflammatory and anti-oxidant activity measured using cotton pellet induce granuloma model. Detection of tumor necrosis factor alpha (TNF α), Interleukin 1 beta (IL-1β), superoxide (SOD), and malondialdehyde (MDA) levels using ELISA Kits. The data analysis by one-way ANOVA followed by the Tukey test. Values are significant at (p < 0.05).

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Publication Date
Thu Dec 29 2016
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of New Symmetrical Pyromellitdiimide Derivatives and Their Amic Acids
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               The new symmetry pyromellitdiimide [VII]a-c,n  were synthesized by two-step reactions from the corresponding pyromellitic dianhydride . A new symmetrical amic acid [VI]a-c,n was synthesized by the reaction of pyromellitic dianhydride with different heterocyclic amines in dry acetone . The second reaction step includes  intramolecular cyclization of amic acid in the presence of  sodium acetate -acetic anhydride system at 850C. Structures  of  the synthesized compounds have been ascertained by their melting points , C.H.N analysis , UV-Vis, FTIR and 1HNMR spectroscopy.

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Publication Date
Tue Feb 02 2021
Journal Name
International Journal Of Pharmaceutical Research
Antimicrobial Evaluation of Some New Synthesized NHydroxy Phthalimide Derivatives
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In this work, N-hydroxy phthalimide derivatives (NHPID) were synthesized from the nucleuphilic substitution reactions of (NHPI) with different halides (alkyl halides, sulfonyl halides, benzoyl halides and benzyl halides). The products were distinguished using FTIR spectrum and Nuclear magnetic resonsnce (1H-NMR and 13CNMR), in addition to other characteristic methods such as sodium fution for sulfur determination. followed by measuring antibacterial (with different types of gram positive/gram negative bacteria) and antifungal activities of these compounds.

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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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Publication Date
Fri Mar 01 2013
Journal Name
Chemistry And Materials Research
Synthesis and Characterization of New Derivatives of Thiazole with Liquid Crystalline properties
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A new two series of liquid crystalline Schiff bases containing thiazole moiety with different length of alkoxy spacer were synthesized, and the relation between the spacer length and the liquid crystalline behavior was investigated. The molecular structures of these compounds were performed by elemental analysis and FTIR, 1HNMR spectroscopy. The liquid crystalline properties were examined by hot stage optical polarizing microscopy (OPM) and differential scanning calorimetry (DSC). All compouns of the two series display liquid crystalline nematic mesophase. The liquid crystalline behaviour has been analyzed in terms of structural property relationship

Publication Date
Tue Jan 01 2019
Journal Name
Journal Of Global Pharma Technology
Synthesis of New Derivatives of Cephalexin with Isatin and Glycine Schiff Bases
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Objectives: Two derivatives of cephalexin were synthesized by reaction with isatin-glycine Schiff base and bromoisatin-glycine Schiff base separately. Methods: Cephalexin was linked through the amine group to isatin glycine and bromoisatin glycine Schiff bases by amide bond formation. Results: These derivatives were characterized by FT-IR, H-NMR, elemental CHN analysis and then tested for their antimicrobial activity compared to cephalexin against gram-positive, gram-negative bacteria and Candida albicans fungi. Conclusion: The two compounds showed better activity against Staphylococcus aureus, compound 3b is more active against Escherichia coli, and compound 3a is more active against Klebsiella pneumonia.

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