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Synthesis and Characterization of some new heterocyclic derivatives from aromatic carbonyl ‎compounds and carboxylic acids with Evaluation some of them for biological activity
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     In this research investigation, a total of eighteen diverse tetra- and penta-lateral cyclic compounds were synthesized. These included 1,3,4-thiadiazole, thiazolidin-4-one (via an alternative method), 1,2,4-triazole, carbothioamide, thiazole-4-one, azetidin-2-one, and oxazole. The synthesis procedure entailed a sequence of reactions. The thiazolidine-4-one 1 was obtained by reaction p-aminobenzoic acid with thiosemicarbazide, followed by treatment with p-tolualdehyde to produce Schiff base 2. Reaction Schiff base 2 with mercaptoacetic acid in dry benzene was carried out to produce thiazolidine-4-one 3. In another synthesis pathway, the esterification of p-nitro benzoic acid with ethanol in the presence of sulfuric acid was obtained to formation of compound 4. Compound 4 was subsequently reacted with thiosemicarbazide, yielding compound 5. Cyclization of compound 5 was then achieved using 4% sodium hydroxide solution. This formed the 1,2,4-triazole heterocycle, designated compound 6. Thiosemicarbazone 7-9 were prepared by reaction of thiosemicarbazide with different aldehydes. Additionally, 2-substituted-1,3-thiazolidine-4-one derivatives 10-12 were synthesized through the reaction of thiosemicarbazone with chloroacetic acid in the presence of anhydrous sodium acetate. The Oxazole derivative 15 was obtained through a series of reactions starting with the reaction of p-amino benzoic acid with ethyl chloroacetate, resulting in compound 13. Compound 13 was then treated with urea to obtain compound 14, followed by a reaction with 4-phenyl phenacyl bromide to yield the final product, the Oxazole derivative 15. The 2-aminooxadiazole derivative 16 was synthesized by reaction urea with 4-bromoacetophenone which was reacted with 4-bromobenzaldehyde to produce Schiff base derivative 17. Finally, β-lactam 18 is obtained through reaction Schiff base with chloroacetyl chloride in the presence of triethyl amine. FT-IR, 1H-NMR, and 13C-NMR spectroscopy were used to confirm their proposed structures. Moreover, the antibacterial and antifungal activities of certain synthesized compounds, specifically 2,3,6,11,13,15,17, and 18, were assessed against Staphylococcus aureus, Escherichia coli, and Candida albicans, demonstrating encouraging outcomes.Keywords: Antibacterial, antifungal activity, oxadaizole, heterocyclic derivatives, Oxazole.

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Publication Date
Wed May 17 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of Some Mixed-Ligand Complexes Containing N-Acetyl Tryptophan and αPicoline with Some Metal Salts
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Some metal ions (Mn+2, Fe+2, Co+2,Ni+2,Cu+2 and Cd+2) complexes of  N-acetyl Tryptophan (AcetrpH) and  α-Picoline (α-Pic) have been synthesized and characterized on the basis of their FTIR,UV-Vis spectroscopy , conductivety measurements , magnetic susceptibility.  From the results obtained, the following general formula has suggested for the prepared complexes.            [M+2(Acetrp)2(α-Pic)2]. XH2O Where  M = Mn+2, Fe+2, Co+2,Ni+2,Cu+2 and Cd+2                         X =  0  ,    0   ,  &nb

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Publication Date
Mon May 22 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Characterization and Effect of bis-1,3,4Oxadiazole Containing Glycine Moiety on the Activity of Some Transferase Enzymes.
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  We described herein the synthesis of novel bis-1,3,4-oxadiazole containing glycine moiety. N-{5-[5-(4-methoxyphenyl)-1,3,4-oxadiazole-2-yl-sulfanyl]-1,3,4-oxadiazole-2-yl-methyl}-4methoxybenzamide was fully characterized by elemental analysis, FT-IR and 1H NMR spectroscopy. Also this study was designed to show the effects of bis-oxadiazole compound on the activities of some transferase enzymes such as: GOT, GPT and γ-GT in sera. This compound demonstrated activation on GOT and GPT activities, inhibitory effects on the γ-GT activity. These effects increased with the increasing of the concentration of the compound. The causes of the increases and decreases in the enzymes activities are discussed

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Publication Date
Sun Nov 21 2021
Journal Name
Iraqi Journal Of Science
Synthesis, Characterization, Biological Activity Studies of Schiff Bases and 1,3-Oxazipene Derived from 1,1 -Bis (4-aminophenyl) -4-Phenyl Cyclohexane
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A series of new Schiff bases and 1, 3-Oxazepine derivatives have been synthesised from condensation compound (1,1 -bis (4-aminophenyl) -4-phenyl cyclohexane [C1] with different aromatic aldehydes in the presence of catalytic glacial acetic acid to produce the Schiff bases [2-4]. These Schiff bases were reacted with maleic anhydride and phthalic anhydride in dry benzene to give seven-membered heterocyclic ring derivatives [5-10].  The structure formula of these compounds were confirmed by using FT-IR, (1H and 13C) NMR spectroscopy. The synthesized compounds were screened for their anti‐bacterial activity using ampicillin as a standard drug.

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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 of Coumarin Derivatives Coupled to Amino Acid Esters and Studying their Biological Activity as Antimicrobial Agents
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A series of coumarin derivatives linked to amino acid ester side chains were synthesized and evaluated of their antibacterial and antifungal activity. The coumarin derivatives was alkylated by the ethyl bromoacetate and then using potassium carbonate to get alkylated hymecromone. Conventional solution method for amide bond formation was used as a coupling method between the carboxy-protected amino acids with acetic acid side chain of coumarin derivatives. The DCC/ HOBt coupling reagents were used for peptide bond formation. The proposed analogues were successfully synthesized and their structural formulas were consistent with the proposed struct

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Publication Date
Thu Dec 28 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Characterization and Antibacterial Activity of New Chalcones Derived from New Aldehyde; 4-[5-(4`tolyl)-1,3,4-thiadiazole-2-yl] benzaldehyde
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 New chalcones of  -{ -  -   -   y  -     - hi di z  e- -y    he y  - -    e e- -  e-    -        - substituted phenyl have been prepared from condensation of  a new of  4-[5-(4`-tolyl)1,3,4-thiadiazole-2-yl] benzaldehyde (which is synthesized by the reaction of  2- amino-5- (4`-tolyl) -1,3,4-thiadiazole and benzaldehyde) with 3- or 4- substituted acetophenones in alkaline medium. The physical, CHNS analysis and spectral data of the synthesized compounds were determined. The biological activity evaluated of new compounds showed that many of these compounds possess antiba

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Publication Date
Sat Dec 30 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis a nd Characterization of Some New Transition Metal Complexes of Amino Thiadiazole
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New complcxcof        Cu (ll),Ni(ll)  ,Co(ll),  and Zn(ll)  wi th 2- amino-5-p-Fiouro Phenyl 1,3,4-Thiadiazole  have been synthesized  . The  products  were isolated , studied  and characterized by physical measurements, i.e., (Ff -IR) ,UV-Vis and  the melting points were determined .The new Schiff base (L) has been used to prepare some complexes  .The   prepared  complexes  were   identified  and   their tructural geometry were suggested.

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Publication Date
Mon Sep 11 2006
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis a nd Characterization of Some New Transition Metal Complexes of Amino Thiadiazole
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New complexes of Cu (ll), Ni (ll), Co (ll), and Zn (ll) wi th 2-amino-5-p-Fiouro Phenyl 1, 3, 4-Thiadiazole have been synthesized. The products were isolated, studied and characterized by physical measurements, ie,(Ff-IR), UV-Vis and the melting points were determined. The new Schiff base (L) has been used to prepare some complexes. The prepared complexes were identified and their structural geometry were suggested

Publication Date
Sun Oct 01 2023
Journal Name
Baghdad Science Journal
Synthesis, characterization, molecular docking, ADMET prediction, and anti-inflammatory activity of some Schiff bases derived from salicylaldehyde as a potential cyclooxygenase inhibitor
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A series of Schiff base-bearing salicylaldehyde moiety compounds (1-4) had been designed, synthesized, subjected to insilico ADMET prediction, molecular docking, characterization by FT-IR, and CHNS analysis techniques, and finally to their Anti-inflammatory profile using cyclooxygenase fluorescence inhibitor screening assay methods along with standard drugs, celecoxib, and diclofenac. The ADMET studies were used to predict which compounds would be suitable for oral administration, as well as absorption sites, bioavailability, TPSA, and drug likeness. According to the results of ADME data, all of the produced chemicals can be absorbed through the GIT and have passed Lipinski’s rule of five. Through molecular docking with PyRx 0.8, these

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Publication Date
Mon Jan 01 2024
Journal Name
Polski Merkuriusz Lekarski
Design, synthesis, insilco study and biological evaluation of new isatin-sulfonamide derivatives by using mono amide linker as possible as histone deacetylase inhibitors
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Aim: To evaluate the cytotoxic activity of newly synthesized a series of novel HDAC inhibitors comprising sulfonamide as zinc binding group and Isatin derivatives as cap group joined by mono amide linker as required to act as HDAC inhibitors. Materials and Methods: The utilization of sulfonamide as zinc binding group joined by N-alkylation reaction with ethyl-bromo hexanoate as linker group that joined by amide reaction with Isatin derivatives as cap groups which known to possess antitumor activity in the designed of new histone deacetylase inhibitors and using the docking and MTT assay to evaluate the compounds. Results: Four compounds have been synthesized and characterized successfully by ART-FTIR, NMR and ESI-Ms. the compounds w

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Publication Date
Tue Aug 02 2011
Journal Name
J. College Of Education / Al-mustansiriya University
Synthesis and characterization of mixed ligand complexes of some metals with ( L- phenylalanine and nicotinamide)
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This paper presents the synthesis and study of some new mixed-ligand complexes containing nicotinamide(C6H7N2O) symbolized (NA) and phenylalanine (C9H11NO2)symbolized (pheH)] with some metal ions. The resulting products were found to be solid crystalline complexes which have been characterized by :Melting points, Solubility, Molar conductivity. determination the percentage of the metal in the complexes by flame(AAS), magnetic susceptipibility, Spectroscopic Method [FT-IR and UV-Vis]. The proposed structure of the complexes using program , chem office 3D(2006) . The general formula have been given for the prepared complexes : [M(NA)2(phe)]cl M(II): Mn(II) ,Co(II) , Ni(II) , Cu(II) , Zn(II) , Cd(II) & Hg(II)). NA = Nicotinamide= C6

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